Reagentia en instrumenten voor immunologie, celbiologie en moleculaire biologie.

Bortezomib [179324-69-7]

Afdrukken

Referentie HY-10227-1ml

Formaat : 10mM/1mL

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Telefoonnummer : +1 850 650 7790

Merk : MedChemExpress

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Telefoonnummer : +1 850 650 7790

Description

Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity^[1]^[2].

IC₅₀ & Target

Ki: 0.6 nM (20S proteasome)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
5TGM1	IC₅₀	6.78 nM Compound: PS-341, Bortezomib	Cytotoxicity against mouse 5TGM1 cells after 48 to 72 hrs by SRB assay Cytotoxicity against mouse 5TGM1 cells after 48 to 72 hrs by SRB assay	[PMID: 24119559]
A2780	IC₅₀	28.9 nM Compound: Bortezomib	Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay	[PMID: 28182990]
A-431	IC₅₀	28.2 nM Compound: Bortezomib	Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay	[PMID: 26231162]
A549	IC₅₀	13.9 nM Compound: bortezomib	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 21077681]
A549	IC₅₀	2.14 μM Compound: Bortezomib	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 28634039]
A549	IC₅₀	2.5 nM Compound: Bortezomib	Antiproliferative activity against human A549 cells after 72 hrs by SRB assay Antiproliferative activity against human A549 cells after 72 hrs by SRB assay	[PMID: 28182990]
A549	IC₅₀	2135.73 nM Compound: PS-341	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: 27769033]
A549	IC₅₀	255 nM Compound: bortezomib	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 19537716]
A549	IC₅₀	6.7 nM Compound: bortezomib	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 20158184]
A549	IC₅₀	9.318 μM Compound: Bortezomib	Antiproliferative activity against human A549 cells after 72 hrs by SRB assay Antiproliferative activity against human A549 cells after 72 hrs by SRB assay	[PMID: 29426629]
A549	IC₅₀	92 nM Compound: BTZ	Antiproliferative activity against human A549 cells after 72 hrs by Cell Titer-Glo assay Antiproliferative activity against human A549 cells after 72 hrs by Cell Titer-Glo assay	[PMID: 28191850]
ARH-77	IC₅₀	6.07 nM Compound: Bortezomib	Cytotoxicity against human ARH77 cells after 72 hrs by MTS assay Cytotoxicity against human ARH77 cells after 72 hrs by MTS assay	[PMID: 26965867]
ARH-77	IC₅₀	9.57 nM Compound: Bortezomib	Cytotoxicity against human ARH77 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay Cytotoxicity against human ARH77 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 29934218]
BEL-7404 tumor cell line	IC₅₀	25.04 nM Compound: PS-341	Antiproliferative activity against human Bel7404 cells after 72 hrs by MTT assay Antiproliferative activity against human Bel7404 cells after 72 hrs by MTT assay	[PMID: 27769033]
BGC-823	IC₅₀	2890 nM Compound: Bortezomib	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 19747832]
BGC-823	IC₅₀	880 nM Compound: bortezomib	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 19537716]
BXPC-3	IC₅₀	11.8 nM Compound: Bortezomib	Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 19747832]
BXPC-3	IC₅₀	16.2 nM Compound: bortezomib	Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 20158184]
BXPC-3	IC₅₀	19.4 nM Compound: bortezomib	Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 21077681]
Calu-6	IC₅₀	3.9 nM Compound: Bortezomib	Inhibition of 26S proteasome beta5 subunit in human Calu6 cells using Suc-LLVY-aminoluciferin as substrate after 1hr by luminescence assay Inhibition of 26S proteasome beta5 subunit in human Calu6 cells using Suc-LLVY-aminoluciferin as substrate after 1hr by luminescence assay	10.1039/C2MD20060K
CCRF-CEM	GI₅₀	0.001 μM Compound: Bortezomib	Antiproliferative activity against human CEM cells after 72 hrs by calcein AM staining based fluorescence assay Antiproliferative activity against human CEM cells after 72 hrs by calcein AM staining based fluorescence assay	[PMID: 28441582]
CCRF-CEM	IC₅₀	11 nM Compound: Bortezomib	Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay	[PMID: 26231162]
DLD-1	IC₅₀	0.0002 μM Compound: Bortezomib, Velcade, PS-341	Inhibition of chymotrypsin-like activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Succinyl-Leu-Leu-Val-Tyr-AMC as substrate after 6 hrs by spectrofluorometric analysis Inhibition of chymotrypsin-like activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Succinyl-Leu-Leu-Val-Tyr-AMC as substrate after 6 hrs by spectrofluorometric analysis	[PMID: 22206869]
DLD-1	IC₅₀	0.0009 μM Compound: Bortezomib, Velcade, PS-341	Inhibition of peptide-glutamyl-peptide-hydrolyzing activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Z-Leu-Leu-Glu-AMC as substrate after 6 hrs by spectrofluorometric analysis Inhibition of peptide-glutamyl-peptide-hydrolyzing activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Z-Leu-Leu-Glu-AMC as substrate after 6 hrs by spectrofluorometric analysis	[PMID: 22206869]
GES1	IC₅₀	12.6 nM Compound: PS-341	Antiproliferative activity against human GES-1 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human GES-1 cells incubated for 48 hrs by MTT assay	[PMID: 32267687]
HCT-116	IC₅₀	0.001 μM Compound: Bortezomib	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 28634039]
HCT-116	IC₅₀	0.01 μM Compound: bortezomib	Cytotoxicity against human HCT116 cells after 72 hrs by CCK-8 assay Cytotoxicity against human HCT116 cells after 72 hrs by CCK-8 assay	[PMID: 23547757]
HCT-116	IC₅₀	1.4 nM Compound: PS-341	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: 27769033]
HCT-116	IC₅₀	27 nM Compound: Bortezomib	Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay	[PMID: 26231162]
HEK293	IC₅₀	0.014 μM Compound: PS-341	Inhibition of NF-kappaB activity in TNF-alpha-induced human HEK293 cells after 30 mins by luciferase assay Inhibition of NF-kappaB activity in TNF-alpha-induced human HEK293 cells after 30 mins by luciferase assay	[PMID: 21044847]
HEK293	IC₅₀	10 nM Compound: 1, bortezomib	Inhibition of TNF-alpha-induced NF-kappaB activation in human HEK293 cells after 3 hrs by luciferase reporter gene assay Inhibition of TNF-alpha-induced NF-kappaB activation in human HEK293 cells after 3 hrs by luciferase reporter gene assay	[PMID: 20875739]
HEK293	IC₅₀	27 nM Compound: 1a, Bortezomib	Inhibition of intracellular chymotrypsin-like activity of 20S proteasome in human HEK293 cells after 24 hrs by fluorescence plate reader Inhibition of intracellular chymotrypsin-like activity of 20S proteasome in human HEK293 cells after 24 hrs by fluorescence plate reader	[PMID: 21634429]
HEK293	CC₅₀	347 nM Compound: 1a, Bortezomib	Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay	[PMID: 21634429]
HEK293	IC₅₀	9.7 nM Compound: Bortezomib	Inhibition of NFkappaB in HEK293 cells incubated for 1 hr prior to TNF-alpha challenge measured after 3 hrs by luciferase reporter gene assay relative to control Inhibition of NFkappaB in HEK293 cells incubated for 1 hr prior to TNF-alpha challenge measured after 3 hrs by luciferase reporter gene assay relative to control	10.1039/C2MD20060K
HEK-293T	IC₅₀	12 nM Compound: BTZ	Antiproliferative activity against human 293T cells after 72 hrs by Cell Titer-Glo assay Antiproliferative activity against human 293T cells after 72 hrs by Cell Titer-Glo assay	[PMID: 28191850]
HeLa	IC₅₀	> 200 nM Compound: Btz	Cytotoxicity against oleic acid-induced human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against oleic acid-induced human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 35059132]
HeLa	IC₅₀	0.02 μM Compound: PS-341	Growth inhibition of human HeLa cells after 72 hrs by MTT assay Growth inhibition of human HeLa cells after 72 hrs by MTT assay	[PMID: 19428245]
HeLa	GI₅₀	168.1 μM Compound: BTZ; Product S4	Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 32031798]
HeLa	IC₅₀	20 nM Compound: Btz	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 35059132]
HeLa	IC₅₀	92 nM Compound: bortezomib	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 19537716]
HepG2	EC₅₀	0.01 μM Compound: Bortezomib	Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29800827]
HepG2	IC₅₀	1.61 nM Compound: PS-341	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 27769033]
HepG2	GI₅₀	100.6 μM Compound: BTZ; Product S4	Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 32031798]
HepG2	IC₅₀	25.2 nM Compound: bortezomib	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 21077681]
HepG2	IC₅₀	37.5 nM Compound: bortezomib	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 19537716]
HepG2	IC₅₀	7.5 nM Compound: bortezomib	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 20158184]
HET-1A	IC₅₀	25.6 nM Compound: PS-341	Antiproliferative activity against human HET-1A cells incubated for 48 hrs by MTT assay Antiproliferative activity against human HET-1A cells incubated for 48 hrs by MTT assay	[PMID: 32267687]
HL-60	ED₅₀	0.0025 μM Compound: Bortezomib	Inhibition of chymotrypsin-like activity of purified human 20S proteasome in HL60 cells using N-succinyl-Leu-Leu-Val-Tyr-AMC as substrate pre-incubated for 10 mins by fluorimetric assay Inhibition of chymotrypsin-like activity of purified human 20S proteasome in HL60 cells using N-succinyl-Leu-Leu-Val-Tyr-AMC as substrate pre-incubated for 10 mins by fluorimetric assay	[PMID: 21973101]
HL-60	IC₅₀	0.008 μM Compound: Bortezomib	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 28634039]
HL-60	ED₅₀	2.5 nM Compound: bortezomib	Inhibition of chymotrypsin-like activity of proteasome in human HL60 cells assessed as free AMC level after 10 mins Inhibition of chymotrypsin-like activity of proteasome in human HL60 cells assessed as free AMC level after 10 mins	[PMID: 19422206]
HL-60	IC₅₀	3.2 nM Compound: Bortezomib	Antiproliferative activity against human HL60 cells after 72 hrs by SRB assay Antiproliferative activity against human HL60 cells after 72 hrs by SRB assay	[PMID: 28182990]
HL-60	IC₅₀	3.5 nM Compound: bortezomib	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 21077681]
HL-60	IC₅₀	5.5 nM Compound: bortezomib	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 19537716]
HL-60	IC₅₀	6.9 nM Compound: Bortezomib	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 19747832]
HL-60	IC₅₀	7.1 nM Compound: bortezomib	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 20158184]
HL-60	IC₅₀	7.6 nM Compound: PS-341	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 27769033]
HT-29	ED₅₀	> 20 μM Compound: Bortezomib	Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay	[PMID: 21973101]
HT-29	IC₅₀	3.2 nM Compound: Btz	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 35059132]
HUVEC	IC₅₀	11.2 nM Compound: PS-341	Antiproliferative activity against HUVEC cells incubated for 48 hrs by MTT assay Antiproliferative activity against HUVEC cells incubated for 48 hrs by MTT assay	[PMID: 32267687]
K562	GI₅₀	0.007 μM Compound: Bortezomib	Antiproliferative activity against human K562 cells after 72 hrs by calcein AM staining based fluorescence assay Antiproliferative activity against human K562 cells after 72 hrs by calcein AM staining based fluorescence assay	[PMID: 28441582]
KB	IC₅₀	59.5 nM Compound: bortezomib	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 19537716]
KM3/BTZ	IC₅₀	226 nM Compound: PS-341	Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay	[PMID: 32267687]
L02	IC₅₀	55.5 nM Compound: PS-341	Antiproliferative activity against human HL7702 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human HL7702 cells incubated for 48 hrs by MTT assay	[PMID: 32267687]
MCF7	IC₅₀	0.025 μM Compound: Bz	Antiproliferative activity against human MCF7 cells after 3 days by SRB assay Antiproliferative activity against human MCF7 cells after 3 days by SRB assay	[PMID: 28557430]
MCF7	IC₅₀	18.37 μM Compound: Bortezomib	Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay	[PMID: 29426629]
MDA-MB-231	IC₅₀	0.003 μM Compound: Bortezomib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	IC₅₀	0.017 μM Compound: Bortezomib	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 28634039]
MDA-MB-231	IC₅₀	16.65 nM Compound: PS-341	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: 27769033]
MDA-MB-231	IC₅₀	3.125 μM Compound: Bortezomib	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 29426629]
MDA-MB-231	IC₅₀	6.5 nM Compound: Bortezomib	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 28182990]
MGC-803	IC₅₀	0.008 μM Compound: Bortezomib	Cytotoxicity against human MGC803 cells after 72 hrs by MTT assay Cytotoxicity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 28634039]
MGC-803	IC₅₀	5.782 nM Compound: PS-341	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 27769033]
MKN-45	IC₅₀	7.15 nM Compound: PS-341	Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 27769033]
MM1.S	IC₅₀	0.0026 μM Compound: Bortezomib	Antiproliferative activity against dexamethasone-sensitive human MM.1S cells assessed as reduction in cell viability measured after 72 hrs by XTT assay Antiproliferative activity against dexamethasone-sensitive human MM.1S cells assessed as reduction in cell viability measured after 72 hrs by XTT assay	[PMID: 34969245]
MM1.S	IC₅₀	0.0032 μM Compound: Bortezomib	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay	[PMID: 36512676]
MM1.S	IC₅₀	2.5 nM Compound: BTZ	Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay	[PMID: 34445874]
MOLT-4	EC₅₀	21 nM Compound: 8	Inhibition of chymotrypsin-like activity of 26S proteasome in human Molt4 cells using MeOSuc-Phe-Leu-Phe-AFC substrate Inhibition of chymotrypsin-like activity of 26S proteasome in human Molt4 cells using MeOSuc-Phe-Leu-Phe-AFC substrate	[PMID: 22503349]
Multiple myeloma cancer stem cell	IC₅₀	8.4 nM Compound: BTZ	Antiproliferative activity against human multiple myeloma cancer stem cells after 72 hrs by MTT assay Antiproliferative activity against human multiple myeloma cancer stem cells after 72 hrs by MTT assay	[PMID: 30108696]
NCI-H23	IC₅₀	0.01 μM Compound: Btz	Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay	[PMID: 30964987]
NCI-H460	IC₅₀	115 nM Compound: bortezomib	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 19537716]
NCI-H460	IC₅₀	780 nM Compound: bortezomib	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 20158184]
NCI-H727	IC₅₀	0.025 μM Compound: Btz	Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay	[PMID: 30964987]
NCI-H929	IC₅₀	10.85 nM Compound: Bortezomib	Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay	[PMID: 24767818]
PBMC	IC₅₀	< 35 nM Compound: Bortezomib	Cytotoxicity against human PBMC after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human PBMC after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30365892]
PBMC	IC₅₀	2.7 nM Compound: 1	Cytotoxicity against human PBMC cells assessed as reduction in cell viability by CellTiter Glo assay Cytotoxicity against human PBMC cells assessed as reduction in cell viability by CellTiter Glo assay	[PMID: 31283222]
PC-3	GI₅₀	0.04 μM Compound: Bortezomib	Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
PC-3	IC₅₀	7 nM Compound: bortezomib	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 20158184]
PC-3	IC₅₀	8.3 nM Compound: bortezomib	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 21077681]
RAW264.7	IC₅₀	0.03 μM Compound: Bortezomib	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of TNFalpha-stimulated NF-kappaB activation by luciferase assay Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of TNFalpha-stimulated NF-kappaB activation by luciferase assay	[PMID: 32738985]
RKO	IC₅₀	20.8 nM Compound: Bortezomib	Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay	[PMID: 26231162]
RPMI-8226	IC₅₀	0.0045 μM Compound: Bortezomib	Antiproliferative activity against human RPMI 8226 cells assessed as reduction in cell viability measured after 72 hrs by XTT assay Antiproliferative activity against human RPMI 8226 cells assessed as reduction in cell viability measured after 72 hrs by XTT assay	[PMID: 34969245]
RPMI-8226	IC₅₀	0.0056 μM Compound: Bortezomib	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay	[PMID: 36512676]
RPMI-8226	IC₅₀	0.0064 μM Compound: BTZ	Antiproliferative activity against human RPMI-8226 cells cultured as 3D-spheroids assessed as reduction in cell viability after 48 hrs by Celltiter-Glo assay Antiproliferative activity against human RPMI-8226 cells cultured as 3D-spheroids assessed as reduction in cell viability after 48 hrs by Celltiter-Glo assay	[PMID: 34445874]
RPMI-8226	IC₅₀	1.43 nM Compound: PS-341	Antiproliferative activity against human RPMI8226 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human RPMI8226 cells incubated for 48 hrs by MTT assay	[PMID: 32267687]
RPMI-8226	IC₅₀	11.2 nM Compound: Bortezomib	Cytotoxicity against human RPMI8226 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay Cytotoxicity against human RPMI8226 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 29934218]
RPMI-8226	IC₅₀	3.88 nM Compound: Bortezomib	Cytotoxicity against human RPMI8226 cells after 72 hrs by MTS assay Cytotoxicity against human RPMI8226 cells after 72 hrs by MTS assay	[PMID: 26965867]
RPMI-8226	IC₅₀	4.7 nM Compound: BTZ	Antiproliferative activity against human RPMI 8226 cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay Antiproliferative activity against human RPMI 8226 cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay	[PMID: 34445874]
RPMI-8226	IC₅₀	6.7 nM Compound: Bortezomib	Antiproliferative activity against human RPMI8226 cells after 72 hrs by SRB assay Antiproliferative activity against human RPMI8226 cells after 72 hrs by SRB assay	[PMID: 28182990]
RPMI-8226	IC₅₀	7.96 nM Compound: Bortezomib	Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay	[PMID: 24767818]
RPMI-8226	IC₅₀	9.5 nM Compound: PS-341, Bortezomib	Cytotoxicity against human RPMI8226 cells after 48 to 72 hrs by SRB assay Cytotoxicity against human RPMI8226 cells after 48 to 72 hrs by SRB assay	[PMID: 24119559]
SK-OV-3	IC₅₀	1.62 nM Compound: PS-341	Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay	[PMID: 27769033]
SK-OV-3	IC₅₀	12.9 nM Compound: Bortezomib	Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 4 days by CellTiter-Glo assay Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 4 days by CellTiter-Glo assay	[PMID: 29767973]
SK-OV-3	IC₅₀	130 nM Compound: bortezomib	Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay	[PMID: 19537716]
SK-OV-3	IC₅₀	151 nM Compound: bortezomib	Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay	[PMID: 20158184]
SK-OV-3	IC₅₀	66.8 nM Compound: bortezomib	Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay	[PMID: 21077681]
SW1990	IC₅₀	79.06 nM Compound: PS-341	Antiproliferative activity against human SW1990 cells after 72 hrs by MTT assay Antiproliferative activity against human SW1990 cells after 72 hrs by MTT assay	[PMID: 27769033]
SW480	IC₅₀	12.3 nM Compound: bortezomib	Cytotoxicity against human SW480 cells after 72 hrs by MTT assay Cytotoxicity against human SW480 cells after 72 hrs by MTT assay	[PMID: 21077681]
SW480	IC₅₀	50 nM Compound: bortezomib	Cytotoxicity against human SW480 cells after 72 hrs by MTT assay Cytotoxicity against human SW480 cells after 72 hrs by MTT assay	[PMID: 19537716]
SW480	IC₅₀	6.1 nM Compound: bortezomib	Cytotoxicity against human SW480 cells after 72 hrs by MTT assay Cytotoxicity against human SW480 cells after 72 hrs by MTT assay	[PMID: 20158184]
TOV21G	IC₅₀	16.7 nM Compound: Bortezomib	Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay	[PMID: 26231162]
U-266	GI₅₀	0.001 μM Compound: Bortezomib	Antiproliferative activity against human U266 cells after 72 hrs by calcein AM staining based fluorescence assay Antiproliferative activity against human U266 cells after 72 hrs by calcein AM staining based fluorescence assay	[PMID: 28441582]
U-266	IC₅₀	11.63 nM Compound: Bortezomib	Cytotoxicity against human U266B1 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay Cytotoxicity against human U266B1 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 29934218]
U-266	IC₅₀	12.2 nM Compound: Bortezomib	Cytotoxicity against human U266 cells after 72 hrs by MTT assay Cytotoxicity against human U266 cells after 72 hrs by MTT assay	[PMID: 19747832]
U-266	IC₅₀	12.5 nM Compound: PS-341	Antiproliferative activity against human U266 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human U266 cells incubated for 48 hrs by MTT assay	[PMID: 32267687]
U-266	IC₅₀	2.45 nM Compound: bortezomib	Cytotoxicity against human U266 cells after 72 hrs by MTT assay Cytotoxicity against human U266 cells after 72 hrs by MTT assay	[PMID: 19537716]
U-266	IC₅₀	5.73 nM Compound: Bortezomib	Cytotoxicity against human U266 cells after 72 hrs by MTS assay Cytotoxicity against human U266 cells after 72 hrs by MTS assay	[PMID: 26965867]
U-266	IC₅₀	8.8 nM Compound: bortezomib	Cytotoxicity against human U266 cells after 72 hrs by MTT assay Cytotoxicity against human U266 cells after 72 hrs by MTT assay	[PMID: 20158184]
WM 266-4	IC₅₀	0.035 μM Compound: Bortezomib, Velcade, PS-341	Cytotoxicity against human WM266.4 cells after 72 hrs by ATPlite assay Cytotoxicity against human WM266.4 cells after 72 hrs by ATPlite assay	[PMID: 22206869]

In Vitro

Bortezomib (PS-341) (100 nM; 8 hours) results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1^[1].
Bortezomib (PS-341) (5-100 nM; 20 hours) induces apoptosis in mantle-cell lymphoma (MCL) cell lines^[3].
Bortezomib (PS-341) (20 nM; 1-14 hours) induces Noxa up-regulation in both MCL cell lines^[3].
The IC₅₀ of Bortezomib (PS-341) is found to be 2.46 nM for 26S proteasome in the B16F10 cells^[4].
Bortezomib (PS-341) suppresses several anti-apoptotic proteins (e.g., Bcl-XL, Bcl-2, and STAT-3)^[5].

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

Cell Cycle Analysis^[1]

Cell Line:	PC-3 cells
Concentration:	100 nM
Incubation Time:	8 hours
Result:	Resulted in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1.

Apoptosis Analysis^[3]

Cell Line:	JVM-2, Granta-519, Jeko, REC-1 cells (MCL cell lines)
Concentration:	5-100 nM
Incubation Time:	20 hours
Result:	The median LD50 for these MCL cell lines was 31 nM (range, 18.2-60.1 nM).

Western Blot Analysis^[3]

Cell Line:	wtp53 (Granta-519), mutp53 (Jeko) cells
Concentration:	20 nM
Incubation Time:	1, 2, 4, 6, 14 hours
Result:	Noxa up-regulation was detected between 2 to 4 hours after bortezomib (PS-341).

In Vivo

Bortezomib (PS-341) (0.3-1 mg/kg; i.v.; once weekly for 4 weeks) inhibits PC-3 Tumor Growth in Nude Mice^[1].

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

Animal Model:	Male nude mice (xenograft tumor model bearing PC-3 cells)^[1]
Dosage:	0.3, 1 mg/kg
Administration:	Intravenous injection; once weekly for 4 weeks
Result:	Resulted in a significant decrease in tumor growth ~60% at dose of 1 mg/kg.

Essai clinique

Masse moléculaire

384.24

Formule

C₁₉H₂₅BN₄O₄

CAS No.

179324-69-7

Appearance

Solid

Color

White to off-white

SMILES

OB(O)[C@H](CC(C)C)NC([C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O

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:

Ethanol : 66.67 mg/mL (173.51 mM; ultrasonic and warming and heat to 60°C)

DMSO : 50 mg/mL (130.13 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	2.6025 mL	13.0127 mL	26.0254 mL
5 mM	0.5205 mL	2.6025 mL	5.2051 mL
10 mM	0.2603 mL	1.3013 mL	2.6025 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, 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.

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: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution

This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (40.0 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 2

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution

This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (40.0 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 3

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution

This protocol yields a clear solution of ≥ 4 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 EtOH stock solution (40.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (6.51 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.51 mM); Clear solution
Protocol 6

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.41 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 7

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.41 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 8

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.41 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.
Protocol 9

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.30 mM); Clear solution

Pureté et documentation

Purity: 99.97%

Fiche technique (282 KB) SDS (557 KB)

COA (251 KB) HNMR (198 KB) LCMS (349 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Adams J, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res. 1999 Jun 1;59(11):2615-22. [Content Brief]

[2]. Shahshahan MA, et al. Potential usage of proteasome inhibitor bortezomib (Velcade, PS-341) in the treatment of metastaticmelanoma: basic and clinical aspects. Am J Cancer Res. 2011;1(7):913-24. [Content Brief]

[3]. Pérez-Galán P, et al. The proteasome inhibitor bortezomib induces apoptosis in mantle-cell lymphoma through generation of ROS and Noxa activation independent of p53 status. Blood. 2006 Jan 1;107(1):257-64. [Content Brief]

[4]. Yerlikaya A, et al. Combined effects of the proteasome inhibitor bortezomib and Hsp70 inhibitors on the B16F10 melanoma cell line. Mol Med Rep. 2010 Mar-Apr;3(2):333-9. [Content Brief]

[5]. Mujtaba T, et al. Advances in the understanding of mechanisms and therapeutic use of bortezomib. Discov Med. 2011 Dec;12(67):471-80. [Content Brief]

[6]. Fernández Y, et al. Chemical blockage of the proteasome inhibitory function of bortezomib: impact on tumor cell death. J Biol Chem. 2006 Jan 13;281(2):1107-18. [Content Brief]

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