HY-10181-100mg | Dasatinib [302962-49-8] Clinisciences

Description

Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The K_is are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively^[1]. Dasatinib also induces apoptosis and autophagy.

IC₅₀ & Target^[1]

Bcr-Abl

1.0 nM (IC₅₀)

Src

0.5 nM (IC₅₀)

lck

0.4 nM (IC₅₀)

yes

0.5 nM (IC₅₀)

c-kit

5.0 nM (IC₅₀)

PDGFRβ

28 nM (IC₅₀)

p38

100 nM (IC₅₀)

Her1

180 nM (IC₅₀)

Her2

710 nM (IC₅₀)

FGFR-1

880 nM (IC₅₀)

MEK

1700 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	8.7 μM Compound: 1, Dasatinib	Cytotoxicity against human A2780 cells after 72 hrs by MTT assay Cytotoxicity against human A2780 cells after 72 hrs by MTT assay	[PMID: 25815152]
A549	IC₅₀	12.66 μM Compound: 3	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 23521020]
A549	IC₅₀	23.73 μM Compound: Dasatinib	Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
A549	IC₅₀	8.2 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human A549 cells after 72 hrs by WST-8 assay Cytotoxicity against human A549 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
A549	IC₅₀	8.37 μM Compound: Dasatinib	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 96 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 27155464]
BaF3	GI₅₀	< 0.0003 μM Compound: Dasatinib	Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	> 1 μM Compound: Dasatinib	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay	[PMID: 26195136]
BaF3	EC₅₀	> 10 μM Compound: Dasatinib	Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay	[PMID: 32657579]
BaF3	EC₅₀	> 10 μM Compound: Dasatinib	Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay	[PMID: 32657579]
BaF3	GI₅₀	> 10 μM Compound: Dasatinib	Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	> 100 nM Compound: Dasatinib	Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay	[PMID: 34011155]
BaF3	EC₅₀	> 1000 nM Compound: Dasatinib	Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 27010810]
BaF3	IC₅₀	0.0002 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.0009 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.001 μM Compound: Dasatinib	Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.001 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	0.0013 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.0019 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.0023 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.003 μM Compound: Dasatinib	Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.003 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	0.0032 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.004 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.005 μM Compound: Dasatinib	Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	0.0051 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.008 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.008 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.01 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.014 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	0.015 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.017 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.017 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	0.019 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.023 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.025 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.029 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	0.039 μM Compound: Dasatinib	Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	EC₅₀	0.04 nM Compound: Dasatinib	Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 27010810]
BaF3	IC₅₀	0.09 μM Compound: Dasatinib	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay	[PMID: 26814890]
BaF3	IC₅₀	0.12 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	0.31 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	0.51 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	0.58 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	0.58 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	0.7 nM Compound: Dasatinib	Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
BaF3	IC₅₀	0.83 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1.29 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1.71 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1.72 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1.91 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1.94 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	1714 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	2.5 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	GI₅₀	3 μM Compound: Dasatinib	Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	3 μM Compound: Dasatinib	Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	3.6 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	3.8 μM Compound: 3	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	4.5 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	5.72 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	6.55 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	6589 nM Compound: 3, BMS-354825	Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	GI₅₀	9.94 μM Compound: Dasatinib	Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BXPC-3	EC₅₀	33 nM Compound: Dasatinib	Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 27010810]
CAKI-2	EC₅₀	55 nM Compound: Dasatinib	Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay	[PMID: 27010810]
CHO	IC₅₀	81.1 μM Compound: dasatinib	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
DLD-1	IC₅₀	4.6 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human DLD1 cells after 72 hrs by WST-8 assay Cytotoxicity against human DLD1 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
DU-145	GI₅₀	0.0623 μM Compound: Dasatinib	Antiproliferative activity against human PRXF DU145 cells after 4 days by modified propidium iodide assay Antiproliferative activity against human PRXF DU145 cells after 4 days by modified propidium iodide assay	[PMID: 25076195]
DU-145	IC₅₀	0.0623 μM Compound: Dasatinib	Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining	[PMID: 23253074]
DU-145	GI₅₀	0.16 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human DU145 cells after 48 hrs by SRB assay Cytotoxicity against human DU145 cells after 48 hrs by SRB assay	[PMID: 24015327]
HCT-116	IC₅₀	2.3 μM Compound: 3	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 23521020]
HCT-116	IC₅₀	3.58 μM Compound: Dasatinib	Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
HCT-116	GI₅₀	3.7 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human HCT116 cells after 48 hrs by SRB assay Cytotoxicity against human HCT116 cells after 48 hrs by SRB assay	[PMID: 24015327]
HCT-116	IC₅₀	5.23 μM Compound: Dasatinib	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 96 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 27155464]
HCT-116	IC₅₀	5.3 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human HCT116 cells after 72 hrs by WST-8 assay Cytotoxicity against human HCT116 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
HEK293	EC₅₀	0.47 μM Compound: Dasatinib	Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay	[PMID: 31520926]
HEK293	IC₅₀	14.3 μM Compound: 1, Dasatinib	Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay	[PMID: 25815152]
HEK293	IC₅₀	63 nM Compound: Dasatinib	Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay	[PMID: 22770610]
HEL	GI₅₀	5.3 μM Compound: Dasatinib	Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
HepG2	IC₅₀	> 5 μM Compound: dasatinib	Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 25835317]
HepG2	IC₅₀	7.5 μM Compound: Dasatinib	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27739679]
HL-60	IC₅₀	14.97 μM Compound: Dasatinib	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
HMEC	GI₅₀	1.8 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human HMEC after 72 hrs by WST1 assay Cytotoxicity against human HMEC after 72 hrs by WST1 assay	[PMID: 24015327]
Hs-578T	GI₅₀	0.03 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human Hs578T cells after 48 hrs by SRB assay Cytotoxicity against human Hs578T cells after 48 hrs by SRB assay	[PMID: 24015327]
JeKo-1	IC₅₀	1325 nM Compound: Dasatinib	Growth inhibition of human Jeko-1 cells incubated for 72 hrs Growth inhibition of human Jeko-1 cells incubated for 72 hrs	[PMID: 33479666]
Jurkat	IC₅₀	> 1000 nM Compound: Dasatinib	Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
K562	GI₅₀	< 0.0003 μM Compound: Dasatinib	Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
K562	IC₅₀	< 1 nM Compound: 13, BMS-354825	Antiproliferative activity against human K562 cells after 72 hrs Antiproliferative activity against human K562 cells after 72 hrs	[PMID: 15615512]
K562	IC₅₀	0.00025 μM Compound: Dasatinib	Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26814890]
K562	GI₅₀	0.0004 μM Compound: BMS-354825	Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay	[PMID: 35944901]
K562	IC₅₀	0.000638 μM Compound: 3	Antiproliferative activity against human K562 cells assessed as reduction in cell viability by measuring ATP level incubated for 3 days by Celltiter-Glo assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability by measuring ATP level incubated for 3 days by Celltiter-Glo assay	[PMID: 31303996]
K562	IC₅₀	0.0007 μM Compound: 3	Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay	[PMID: 23521020]
K562	IC₅₀	0.001 μM Compound: Dasatinib	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
K562	IC₅₀	0.001 μM Compound: Dasatinib	Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay	[PMID: 26195136]
K562	IC₅₀	0.19 nM Compound: Dasatinib	Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay	[PMID: 32657579]
K562	IC₅₀	0.2 nM Compound: Dasatinib	Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34011155]
K562	CC₅₀	0.25 μM Compound: VI	Cytotoxicity against human K562 cells assessed as decrease in cell viability by MTT assay Cytotoxicity against human K562 cells assessed as decrease in cell viability by MTT assay	[PMID: 27474918]
K562	IC₅₀	0.45 μM Compound: BMS-354825	Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 26451772]
K562	IC₅₀	0.9 nM Compound: Dasatinib	Growth inhibition of human K562 cells incubated for 2 days by CCK8 assay Growth inhibition of human K562 cells incubated for 2 days by CCK8 assay	[PMID: 31539241]
K562	IC₅₀	0.9 nM Compound: Dasatinib	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34217059]
K562	IC₅₀	1 nM Compound: 2, dasatinib,BMS-354825	Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay	[PMID: 17956080]
K562	IC₅₀	11.9 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human K562 cells after 72 hrs by WST-8 assay Cytotoxicity against human K562 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
K562	IC₅₀	11.95 μM Compound: Dasatinib	Cytotoxicity against human K562 cells assessed as reduction in cell viability after 96 hrs by MTT assay Cytotoxicity against human K562 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 27155464]
K562	IC₅₀	12.83 μM Compound: BMS-354825, SPRYCEL	Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay	[PMID: 22217877]
K562	GI₅₀	9.7 μM Compound: BMS-354825	Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay	[PMID: 35944901]
KM12	GI₅₀	7.44 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human KM12 cells after 48 hrs by SRB assay Cytotoxicity against human KM12 cells after 48 hrs by SRB assay	[PMID: 24015327]
KU812 cell line	GI₅₀	< 0.0003 μM Compound: Dasatinib	Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
KU812 cell line	IC₅₀	0.1 nM Compound: Dasatinib	Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
L02	IC₅₀	> 40 μM Compound: Dasatinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability after 96 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 27155464]
Malme-3M	GI₅₀	6.61 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human MALME-3M cells after 48 hrs by SRB assay Cytotoxicity against human MALME-3M cells after 48 hrs by SRB assay	[PMID: 24015327]
Maver1	IC₅₀	1325 nM Compound: Dasatinib	Growth inhibition of human MAVER-1 cells incubated for 72 hrs Growth inhibition of human MAVER-1 cells incubated for 72 hrs	[PMID: 33479666]
MCF7	IC₅₀	1.11 μM Compound: Dasatinib	Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
MCF7	IC₅₀	2.57 μM Compound: 3	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 23521020]
MCF7	IC₅₀	8.05 μM Compound: 1a	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25899332]
MCF7	GI₅₀	8.32 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 24015327]
MDA-MB-231	GI₅₀	0.02 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay	[PMID: 24015327]
MDA-MB-231	IC₅₀	0.112 μM Compound: Dasatinib	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27739679]
MDA-MB-231	IC₅₀	0.178 μM Compound: dasatinib	Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 25835317]
MDA-MB-231	IC₅₀	1.12 μM Compound: 1a	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25899332]
MDA-MB-231	IC₅₀	12 nM Compound: 13, BMS-354825	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs	[PMID: 15615512]
MDA-MB-231	EC₅₀	44 nM Compound: Dasatinib	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 27010810]
MDA-MB-435	IC₅₀	5.147 μM Compound: Dasatinib	Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27739679]
MDA-MB-435S	IC₅₀	3.9 μM Compound: 3	Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay	[PMID: 23521020]
MEG-01	GI₅₀	< 0.0003 μM Compound: Dasatinib	Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
MOLM-14	GI₅₀	2.3 μM Compound: Dasatinib	Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
MV4-11	GI₅₀	3.6 μM Compound: Dasatinib	Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
NCI-H1975	EC₅₀	173 nM Compound: Dasatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 27010810]
NCI-H2286	IC₅₀	0.032 μM Compound: Dasatinib	Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay	[PMID: 26191369]
NCI-H2286	IC₅₀	33.3 nM Compound: Dasatinib	Antiproliferative activity against human NCI-H2286 cells harboring DDR2 mutation after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H2286 cells harboring DDR2 mutation after 72 hrs by CCK8 assay	[PMID: 30572178]
NCI-H23	IC₅₀	2.27 μM Compound: 3	Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay	[PMID: 23521020]
NCI-H460	IC₅₀	8.99 μM Compound: 3	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 23521020]
NCI-H661	IC₅₀	7.8 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human NCI-H661 cells after 72 hrs by WST-8 assay Cytotoxicity against human NCI-H661 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
NHDF	IC₅₀	0.71 μM Compound: Dasatinib	Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
PC-3	EC₅₀	232 nM Compound: Dasatinib	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 27010810]
PC-3	IC₅₀	9.4 nM Compound: 13, BMS-354825	Antiproliferative activity against human PC3 cells after 72 hrs Antiproliferative activity against human PC3 cells after 72 hrs	[PMID: 15615512]
SW-620	GI₅₀	8.43 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human SW620 cells after 48 hrs by SRB assay Cytotoxicity against human SW620 cells after 48 hrs by SRB assay	[PMID: 24015327]
T47D	IC₅₀	0.9 μM Compound: 3	Antiproliferative activity against human T47D cells after 72 hrs by MTT assay Antiproliferative activity against human T47D cells after 72 hrs by MTT assay	[PMID: 23521020]
U-251	GI₅₀	2.81 μM Compound: Sprycel, NSC 723517	Cytotoxicity against human U251 cells after 48 hrs by SRB assay Cytotoxicity against human U251 cells after 48 hrs by SRB assay	[PMID: 24015327]
U-937	GI₅₀	> 10 μM Compound: Dasatinib	Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
U-937	IC₅₀	> 1000 nM Compound: Dasatinib	Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
U-937	IC₅₀	≥ 100 nM Compound: dasatinib	Inhibition of LPS-induced Btk autophosphorylation on Tyr223 in human U937 cells at >= 100 nM after 1 hr Inhibition of LPS-induced Btk autophosphorylation on Tyr223 in human U937 cells at >= 100 nM after 1 hr	[PMID: 17684099]
U-937	IC₅₀	10.23 μM Compound: Dasatinib	Cytotoxicity against human U937 cells assessed as reduction in cell viability after 96 hrs by MTT assay Cytotoxicity against human U937 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 27155464]
U-937	IC₅₀	12.2 μM Compound: Dasatinib, BMS-354825	Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay	[PMID: 23567960]
U-937	IC₅₀	13.63 μM Compound: BMS-354825, SPRYCEL	Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay	[PMID: 22217877]
U-937	IC₅₀	15.02 μM Compound: Dasatinib	Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 36242991]
WiDr	IC₅₀	52 nM Compound: 13, BMS-354825	Antiproliferative activity against human WiDr cells after 72 hrs Antiproliferative activity against human WiDr cells after 72 hrs	[PMID: 15615512]

In Vitro

Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC₅₀s of <1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively^[1].
Dasatinib shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC₅₀s of <1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels^[1].
Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t_1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (F_po) in this study is 27%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mice bearing K562 xenografts
Dosage:	5 mg/kg and 50 mg/kg
Administration:	Oral administration on a 5 day on and 2 day off schedule.
Result:	Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.

Animal Model:	Sprague-Dawley Rats
Dosage:	10 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral and i.v.
Result:	C_max of 13.2 and 0.5 μM for i.v. and oral, respectively.

Essai clinique

Masse moléculaire

488.01

Formule

C₂₂H₂₆ClN₇O₂S

CAS No.

302962-49-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN=C(S1)NC2=NC(C)=NC(N3CCN(CC3)CCO)=C2)NC4=C(C=CC=C4Cl)C

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (256.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0491 mL	10.2457 mL	20.4914 mL
5 mM	0.4098 mL	2.0491 mL	4.0983 mL
10 mM	0.2049 mL	1.0246 mL	2.0491 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité
Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 50 mg/mL (102.46 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 20% SBE-β-CD in Saline
Solubility: 2 mg/mL (4.10 mM); Suspended solution; Need ultrasonic
Protocol 3

Add each solvent one by one: 0.5% Methyl cellulose/0.5% Tween-80 in Saline water
Solubility: 6.67 mg/mL (13.67 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureté et documentation

Purity: 99.88%

Select Batch:

SDS (393 KB)

COA (247 KB) HNMR (284 KB) RP-HPLC (243 KB) LCMS (93 KB) Elemental Analysis Report (104 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Lombardo LJ, et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004 Dec 30;47(27):6658-61. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0491 mL	10.2457 mL	20.4914 mL	51.2285 mL
	5 mM	0.4098 mL	2.0491 mL	4.0983 mL	10.2457 mL
	10 mM	0.2049 mL	1.0246 mL	2.0491 mL	5.1228 mL
	15 mM	0.1366 mL	0.6830 mL	1.3661 mL	3.4152 mL
	20 mM	0.1025 mL	0.5123 mL	1.0246 mL	2.5614 mL
	25 mM	0.0820 mL	0.4098 mL	0.8197 mL	2.0491 mL
	30 mM	0.0683 mL	0.3415 mL	0.6830 mL	1.7076 mL
	40 mM	0.0512 mL	0.2561 mL	0.5123 mL	1.2807 mL
	50 mM	0.0410 mL	0.2049 mL	0.4098 mL	1.0246 mL
	60 mM	0.0342 mL	0.1708 mL	0.3415 mL	0.8538 mL
	80 mM	0.0256 mL	0.1281 mL	0.2561 mL	0.6404 mL
	100 mM	0.0205 mL	0.1025 mL	0.2049 mL	0.5123 mL

Dasatinib Related Classifications

Protein Tyrosine Kinase/RTK Autophagy Apoptosis
Bcr-Abl Src Autophagy Apoptosis

Dasatinib [302962-49-8]

Cat# HY-10181-100mg

Contatta il distributore locale :

Marca : MedChemExpress

Contatta il distributore locale :

Other Forms of Dasatinib:

Voir tous les produits spécifiques à Isoform Src:

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Dasatinib Related Classifications

Keywords:

Si può anche essere interessati nei seguenti prodotti:

Dasatinib [302962-49-8]

Cat# HY-10181-100mg

Contatta il distributore locale :

Marca : MedChemExpress

Contatta il distributore locale :

Other Forms of Dasatinib:

Voir tous les produits spécifiques à Isoform Src:

Dasatinib Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Dasatinib Related Classifications

Keywords:

Si può anche essere interessati nei seguenti prodotti: