HY-16297A-5mg | Abemaciclib [1231929-97-7] Clinisciences

Description

Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

IC₅₀ & Target^[3]

Cdk4/cyclin D1

2 nM (IC₅₀)

CDK6/cyclinD1

10 nM (IC₅₀)

CDK9/cyclinT1

57 nM (IC₅₀)

CDK5/p35

287 nM (IC₅₀)

Cdk5/p25

355 nM (IC₅₀)

CDK2/cyclinE

504 nM (IC₅₀)

CDK1/cyclinB1

1627 nM (IC₅₀)

CDK7/Mat1/cyclinH1

3910 nM (IC₅₀)

PIM1

50 nM (IC₅₀)

PIM2

3400 nM (IC₅₀)

HIPK2

31 nM (IC₅₀)

DYRK2

61 nM (IC₅₀)

CK2

117 nM (IC₅₀)

GSK3b

192 nM (IC₅₀)

JNK3

389 nM (IC₅₀)

FLT3 (D835Y)

403 nM (IC₅₀)

DRAK1

659 nM (IC₅₀)

FLT3

3960 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A 172	EC₅₀	0.2 μM Compound: 3	Antiproliferative activity against human A172 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human A172 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
A549	IC₅₀	253 nM Compound: Abemaciclib	Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
COLO 205	IC₅₀	0.217 μM Compound: Abemaciclib	Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay	[PMID: 29459274]
COLO 205	IC₅₀	0.46 μM Compound: LY2835219	Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay	[PMID: 29074254]
COLO 205	IC₅₀	120 nM Compound: LY-2835219	Inhibition of CDK4/6 in human COLO205 cells assessed as inhibition of Rb phosphorylation after 24 hrs by propidium iodide staining-based laser-scanning fluorescence microplate cytometric analysis Inhibition of CDK4/6 in human COLO205 cells assessed as inhibition of Rb phosphorylation after 24 hrs by propidium iodide staining-based laser-scanning fluorescence microplate cytometric analysis	[PMID: 26115571]
COLO 205	IC₅₀	253 nM Compound: Abemaciclib	Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
COLO 205	IC₅₀	253 nM Compound: Abemaciclib	Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
CWR22R	GI₅₀	0.348 μM Compound: Abemaciclib	Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
DBTRG-05MG	EC₅₀	0.19 μM Compound: 3	Antiproliferative activity against human DBTRG-05MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human DBTRG-05MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
EMT6	IC₅₀	4.18 μM Compound: Abemaciclib	Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35447031]
HEK293	GI₅₀	10.925 μM Compound: Abemaciclib	Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
HeLa	IC₅₀	768 nM Compound: Abemaciclib	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
HL-60	GI₅₀	0.664 μM Compound: Abemaciclib	Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
HT-22	IC₅₀	12.2 μM Compound: 1	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]
HUVEC	IC₅₀	403 nM Compound: Abemaciclib	Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
Jurkat	GI₅₀	4.63 μM Compound: Abemaciclib	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
K562	GI₅₀	0.624 μM Compound: Abemaciclib	Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
M059J	EC₅₀	9.24 μM Compound: 3	Antiproliferative activity against human M059J assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human M059J assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
MCF-10A	GI₅₀	5.088 μM Compound: Abemaciclib	Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
MCF7	GI₅₀	0.832 μM Compound: Abemaciclib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
MCF7	GI₅₀	4.01 μM Compound: Abemaciclib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
MCF7	IC₅₀	99.8 nM Compound: Abemaciclib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
MDA-MB-231	IC₅₀	> 20 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35447031]
MDA-MB-231	IC₅₀	191 nM Compound: LY2835219	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay	[PMID: 29429832]
MDA-MB-231	GI₅₀	3.45 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
MDA-MB-231	IC₅₀	62 nM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
MDA-MB-468	IC₅₀	> 20 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35447031]
MDA-MB-468	IC₅₀	1144 nM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
MDA-MB-468	IC₅₀	4.808 μM Compound: Abemaciclib	Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay	[PMID: 29459274]
MIA PaCa-2	IC₅₀	5.8 μM Compound: Abemaciclib	Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay	[PMID: 33316409]
RPMI-8226	GI₅₀	1.479 μM Compound: Abemaciclib	Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
SF-539	EC₅₀	3.22 μM Compound: 3	Antiproliferative activity against human SF539 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human SF539 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
Sf9	IC₅₀	0.005 μM Compound: Abemaciclib	Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.01 μM Compound: Abemaciclib	Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	0.065 μM Compound: Abemaciclib	Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	0.101 μM Compound: Abemaciclib	Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.273 μM Compound: Abemaciclib	Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	0.347 μM Compound: Abemaciclib	Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.371 μM Compound: LY2835219	Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP	[PMID: 26741853]
Sf9	IC₅₀	0.371 μM Compound: Abemaciclib	Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	0.405 μM Compound: Abemaciclib	Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
Sf9	IC₅₀	3.1 μM Compound: Abemaciclib	Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay	[PMID: 30234987]
SiHa	IC₅₀	861 nM Compound: Abemaciclib	Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
T47D	GI₅₀	0.771 μM Compound: Abemaciclib	Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay	[PMID: 36350721]
T47D	IC₅₀	145 nM Compound: Abemaciclib	Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
T47D	IC₅₀	34.3 nM Compound: Abemaciclib	Antiproliferative activity against human T47D cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human T47D cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]
T98G	EC₅₀	0.54 μM Compound: 3	Antiproliferative activity against human T98G assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human T98G assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
U-266	GI₅₀	2.701 μM Compound: Abemaciclib	Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 34875521]
U-87MG ATCC	EC₅₀	0.12 μM Compound: 3	Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay	[PMID: 31307887]
U-87MG ATCC	IC₅₀	48.1 nM Compound: Amebaciclib	Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay	[PMID: 29247857]
U-87MG ATCC	IC₅₀	706 nM Compound: Abemaciclib	Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay	[PMID: 32200202]
Vero	CC₅₀	> 50 μM Compound: Abemaciclib	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	6.62 μM Compound: Abemaciclib	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730
ZR-75-1	IC₅₀	83.4 nM Compound: Abemaciclib	Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay	[PMID: 31200237]

In Vitro

Abemaciclib reduces cell viability with the IC₅₀ values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells^[1]. Abemaciclib shows inhibition on A375R1-4, M14R, and SH4R with EC₅₀ values ranging from 0.3 to 0.6 μM; Abemaciclib inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC₅₀ values of 395, 260, and 463 nM, respectively^[2]. Abemaciclib inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells^[3].

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

In Vivo

Abemaciclib (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor^[1]. Abemaciclib (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model^[2].

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

Essai clinique

Masse moléculaire

506.59

Formule

C₂₇H₃₂F₂N₈

CAS No.

1231929-97-7

Appearance

Solid

Color

Off-white to yellow

SMILES

CC1=NC2=C(F)C=C(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)C=C2N1C(C)C

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvant et solubilité

In Vitro:

DMSO : 2.94 mg/mL (5.80 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9740 mL	9.8699 mL	19.7398 mL
5 mM	0.3948 mL	1.9740 mL	3.9480 mL
10 mM	---	---	---

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo:

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% Hydroxyethyl cellulose in Water
Solubility: 3.33 mg/mL (6.57 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

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Pureté et documentation

Purity: 99.97%

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SDS (419 KB)

COA (244 KB) HNMR (232 KB) RP-HPLC (245 KB) MS (211 KB) Elemental Analysis Report (102 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget.?2016 Mar 22;7(12):14803-13. [Content Brief]

[2]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63. [Content Brief]

[3]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37. [Content Brief]

Test cellulaire ^[1]	Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between Abemaciclib and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of <1 is synergistic and a CI of >1 is antagonistic. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Administration animale ^[1]	Six-week-old BALB/c female nude mice are injected subcutaneously with OSC-19 (1×10⁶) cells. When tumor sizes reach approximately 100 mm³, mice are randomized by tumor size and subjected to each treatment. At least 5 mice per treatment group are included. Each group of mice is dosed via daily oral gavage with vehicle, Abemaciclib (45 mg/kg/d or 90 mg/kg/d), RAD001 (5 mg/kg/d), or a combination of both. The Abemaciclib is dissolved in 1% HEC in 20 mM phosphate buffer (pH2.0). Tumor size and body weight are measured twice weekly. Tumor volumes are calculated using the following formula: V=(L×W²)/2. Mice are gavaged a final time on day 14 and sacrificed the following day. The tumors are removed for Western blot and immunohistochemistry. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références	[1]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget.?2016 Mar 22;7(12):14803-13. [Content Brief] [2]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63. [Content Brief] [3]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9740 mL	9.8699 mL	19.7398 mL	49.3496 mL
DMSO	5 mM	0.3948 mL	1.9740 mL	3.9480 mL	9.8699 mL

Abemaciclib Related Classifications

Cell Cycle/DNA Damage
CDK

Abemaciclib [1231929-97-7]

Referência HY-16297A-5mg

Contactar o distribuidor local :

Marca : MedChemExpress

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Abemaciclib Related Classifications

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Abemaciclib [1231929-97-7]

Referência HY-16297A-5mg

Contactar o distribuidor local :

Marca : MedChemExpress

Contactar o distribuidor local :

Other Forms of Abemaciclib:

Voir tous les produits spécifiques à Isoform CDK:

Abemaciclib Related Antibodies

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Complete Stock Solution Preparation Table

Abemaciclib Related Classifications

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