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ABT-737 Bcl-2 Inhibiteur

Name: ABT-737
Brand: Selleck Chemicals
SKU: S1002
Rating: 5 (384 reviews)

N° Cat.S1002

ABT-737 est un inhibiteur mimétique de BH3 de Bcl-xL, Bcl-2 et Bcl-w avec une EC50 de 78,7 nM, 30,3 nM et 197,8 nM dans des essais sans cellules, respectivement; aucune inhibition observée contre Mcl-1, Bcl-B ou Bfl-1. ABT-737 induit l'Apoptosis par voie mitochondriale et la Mitophagy. Phase 2.

ABT-737 Bcl-2 inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 813.43

Aller à

Contrôle qualité

Lot : Pureté : 99.99%

99.99

Cibles apparentées	Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Autre Bcl-2 Inhibiteurs	Navitoclax (ABT-263) S63845 Obatoclax Mesylate (GX15-070) A-1331852 A-1210477 TW-37 A-1155463 Dihydrochloride AZD5991 UMI-77 (R)-(-)-Gossypol (AT-101) acetic acid

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Formulation	Description de lactivité	PMID
OCI-Ly1	Cell Viability Assay	250 nM	72 h	DMSO	caused 97% loss of viability in cells transfected with BCL6 siRNA	26657288
KG1a	Cell Viability Assay	0-10 μM	24 h	DMSO	IC50=7.68 μM, decreases cell viability in a dose-dependent manner	26552712
Kasumi-1	Cell Viability Assay	0-10 μM	24 h	DMSO	IC50=4.87 μM, decreases cell viability in a dose-dependent manner	26552712
KG1a	Apoptosis Assay	0-10 μM	24 h	DMSO	induces cell apoptosis in a dose-dependent manner	26552712
Kasumi-1	Apoptosis Assay	0-10 μM	24 h	DMSO	induces cell apoptosis in a dose-dependent manner	26552712
MC-3	Growth Inhibition Assay	5/10/20 μM	24 h	DMSO	inhibits cell growth in a dose-dependent manner	26447615
HN22	Growth Inhibition Assay	2.5/7.5/22.5 μM	24 h	DMSO	inhibits cell growth in a dose-dependent manner	26447615
MC-3	Apoptosis Assay	5/10/20 μM	24 h	DMSO	induces caspase-mediated apoptosis	26447615
HN22	Apoptosis Assay	2.5/7.5/22.5 μM	24 h	DMSO	induces caspase-mediated apoptosis	26447615
MOLT-4	Growth Inhibition Assay	10-5000 nM	72 h	DMSO	IC50=0.198 μM	26392332
RS4;11	Growth Inhibition Assay	10-5000 nM	72 h	DMSO	IC50=0.002 μM	26392332
JURKAT	Growth Inhibition Assay	10-5000 nM	72 h	DMSO	IC50=66 μM	26392332
CEM R	Growth Inhibition Assay	10-5000 nM	72 h	DMSO	IC50=5.4 μM	26392332
CEM S	Growth Inhibition Assay	10-5000 nM	72 h	DMSO	IC50=12.1 μM	26392332
MOLT-4	Apoptosis Assay	10-1000 nM	24 h	DMSO	causes the cleavage of Bcl-2 and the downregulation of Bcl-xL and Mcl-1	26392332
CEM S	Apoptosis Assay	10-1000 nM	24 h	DMSO	causes the cleavage of Bcl-2 and the downregulation of Bcl-xL and Mcl-1	26392332
JURKAT	Growth Inhibition Assay	100-1000 nM	48 h	DMSO	IC50=955±9.3 nM	26172269
LOUCY	Growth Inhibition Assay	100-1000 nM	48 h	DMSO	IC50=32.8±10.9 nM	26172269
WM-115	Cell Viability Assay	100 nM	72 h		enhances curcumin-induced anti-survival	26116776
B16	Cell Viability Assay	100 nM	72 h		enhances curcumin-induced anti-survival	26116776
HL-60	Growth Inhibition Assay		72 h		IC50 = 10.7 nM	26045609
MOLM-13	Growth Inhibition Assay		72 h		IC50 = 27.9 nM	26045609
OCI-AML3	Growth Inhibition Assay		72 h		IC50 = 1950 nM	26045609
BCWM.1	Apoptosis Assay	0-1.6 μM	24 h		induces cell apoptosis	25893290
MWCL-1	Apoptosis Assay	0-1.6 μM	24 h		induces cell apoptosis	25893290
MM.1s	Apoptosis Assay	0-1.6 μM	24 h		induces cell apoptosis	25893290
HCT116	Function Assay	3/10 μM	12 h	DMSO	induces a dose-dependent increase in LC3B-II conversion and SQSTM1 degradation	25715028
HCT116 BAX BAK1 DKO	Function Assay	3/10 μM	12 h	DMSO	induces a dose-dependent increase in LC3B-II conversion and SQSTM1 degradation	25715028
HCT116	Function Assay	10 μM	12 h	DMSO	increases GFP-LC3B puncta	25715028
HCT116 BAX BAK1 DKO	Function Assay	10 μM	12 h	DMSO	increases GFP-LC3B puncta	25715028
HCT116	Autophagy Assay	10 μM	12 h	DMSO	induces a complete autophagic response	25715028
HCT116 BAX BAK1 DKO	Autophagy Assay	10 μM	12 h	DMSO	induces a complete autophagic response	25715028
U937	Apoptosis Assay	0.125-2 μM	24 h		enhances DHA/X-11-induced apoptosis	25714024
U937	Apoptosis Assay	0.5 μM	24 h		enhances cleavage of PARP and caspase-3 as well as Noxa level	25714024
HL-60 AAA-Bcl-2	Apoptosis Assay	0-5 μM	48 h		IC50=0.87 μm，induces cell apoptosis in a dose-dependent manner	25711460
HL-60 EEE-Bcl-2	Apoptosis Assay	0-5 μM	48 h		IC50=5 μm， induces cell apoptosis in a dose-dependent manner	25711460
U87	Function Assay	50 μM	24 h		reduces the mRNA expression levels of MMP-2, MMP-14 and Bcl-2	25667663
K562	Cell Viability Assay	1-10 μM	48 h	DMSO	IC50=26.7 μM	25596561
K562/Mcl -1-IRESBim	Growth Inhibition Assay				IC50=9.3 μM	25535900
K562/Bcl- 2-IRESBim	Growth Inhibition Assay				IC50=0.35 μM	25535900
Jurkat	Growth Inhibition Assay				IC50=0.66 μM	25535900
JurkatΔBak	Growth Inhibition Assay				IC50>50 μM	25535900
HL60/VCR	Growth Inhibition Assay				IC50>100 μM	25535900
Kasumi-1	Growth Inhibition Assay				IC50=0.01 μM	25535900
Kasumi-1/ABT	Growth Inhibition Assay				IC50=0.51 μM	25535900
THP-1	Growth Inhibition Assay				IC50=1.27 μM	25535900
U937	Growth Inhibition Assay				IC50=5.29 μM	25535900
C1498	Growth Inhibition Assay				IC50=6.13 μM	25535900
RPMI 8226	Growth Inhibition Assay				IC50=0.25 μM	25535900
MM.1S	Growth Inhibition Assay				IC50=0.40 μM	25535900
NCI-H929	Growth Inhibition Assay				IC50=15.21 μM	25535900
U266	Growth Inhibition Assay				IC50=0.68 μM	25535900
MCF-7	Cell Viability Assay	5 μM	48 h	DMSO	enhances the sensitivity to or radiation	25409124
MCF-7	Apoptosis Assay	5 μM	4/24/48 h	DMSO	increases the cleaved PARP	25409124
MCF-7	Function Assay	5 μM	24 h	DMSO	enhances thelevel of Mcl-1 expression	25409124
MDA-MB 231	Function Assay	5 μM	24 h	DMSO	enhances thelevel of Mcl-1 expression	25409124
ZR-75-1	Function Assay	5 μM	24 h	DMSO	enhances thelevel of Mcl-1 expression	25409124
A549	Cell Viability Assay	0-20 μM	72 h	DMSO	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
H1299	Cell Viability Assay	0-20 μM	72 h	DMSO	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
HO-8910	Cell Viability Assay	0-20 μM	72 h	DMSO	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
HT-29	Cell Viability Assay	0-20 μM	72 h	DMSO	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
HCT-116	Cell Viability Assay	0-20 μM	72 h	DMSO	decreases the cell survival in a dose-dependent manner combined with aspirin	25388762
A549	Apoptosis Assay	20 μM	48 h	DMSO	induces apoptosis significantly combined with aspirin	25388762
H1299	Apoptosis Assay	20 μM	48 h	DMSO	induces apoptosis significantly combined with aspirin	25388762
Sc-1	Cell Viability Assay	0.0001-1 μM	96 h		decreases the cell viability in a dose-dependent manner	25373508
OcI-LY18	Cell Viability Assay	0.0001-1 μM	96 h		decreases the cell viability in a dose-dependent manner	25373508
RL	Cell Viability Assay	0.0001-1 μM	96 h		decreases the cell viability in a dose-dependent manner	25373508
RKO	Cell Viability Assay	0-10 μM	24 h	DMSO	IC50> 25 µM	25304383
Caco-2	Cell Viability Assay	0-10 μM	24 h	DMSO	IC50=19.7 µM	25304383
DLD1	Cell Viability Assay	0-10 μM	24 h	DMSO	IC50=18.78 µM	25304383
LS411N	Cell Viability Assay	0-10 μM	24 h	DMSO	IC50=11.47 µM	25304383
SW620	Cell Viability Assay	0-10 μM	24 h	DMSO	IC50=12.24 µM	25304383
HCT116	Cell Viability Assay	0-10 μM	24 h	DMSO	IC50=20.49 µM	25304383
HaCaT	Cell Viability Assay	0.1/1/10 μM	24 h	DMSO	decreases cell viability in a dose-dependent manner	25210795
A5-RT3	Cell Viability Assay	0.1/1/10 μM	24 h	DMSO	decreases cell viability in a dose-dependent manner	25210795
HaCaT	Function Assay	10 μM	24/48 h	DMSO	induces MMP and DNA fragmentation	25210795
A5-RT3	Function Assay	10 μM	24/48 h	DMSO	induces MMP and DNA fragmentation	25210795
A5-RT3	Function Assay	5 μM	6 h	DMSO	induces the release of mitochondrial proteins and reduces clonogenic survival in a caspase-independent manner	25210795
U266	Function Assay	500/750 nM	24/48 h	DMSO	downregulates Bim, principally the EL isoform	25208888
RPMI8226	Function Assay	500/750 nM	24/48 h	DMSO	downregulates Bim, principally the EL isoform	25208888
MM.1S	Function Assay	500/750 nM	24/48 h	DMSO	downregulates Bim, principally the EL isoform	25208888
Clone A	Growth Inhibition Assay	0.2–60 μM	72 h	DMSO	IC50=7.5 μM	25208882
CX-1	Growth Inhibition Assay	0.2–60 μM	72 h	DMSO	IC50=1.8 μM	25208882
LS174T	Growth Inhibition Assay	0.2–60 μM	72 h	DMSO	IC50=18.3 μM	25208882
HT29	Apoptosis Assay	1/5/10 μM	48 h		causes cell death in a dose-dependent manner	25192188
SW480	Apoptosis Assay	1/5/10 μM	48 h		causes cell death in a dose-dependent manner	25192188
Colo205	Apoptosis Assay	1/5/10 μM	48 h		causes cell death in a dose-dependent manner	25192188
Caco2	Apoptosis Assay	1/5/10 μM	48 h		causes cell death in a dose-dependent manner	25192188
PCI-13	Growth Inhibition Assay		72 h	DMSO	GI50=15 ± 1.8 μM	25139387
PCI-15B	Growth Inhibition Assay		72 h	DMSO	GI50=11 ± 4.5 μM	25139387
UM-SCC22B	Growth Inhibition Assay		72 h	DMSO	GI50=19 ± 2.9 μM	25139387
UM-SCC47	Growth Inhibition Assay		72 h	DMSO	GI50=19 ± 12.3 μM	25139387
93-VU-147T	Growth Inhibition Assay		72 h	DMSO	GI50=4.3 ± 3.5 μM	25139387
UD-SCC2	Growth Inhibition Assay		72 h	DMSO	GI50=28 ± 2.9 μM	25139387
UPCI:SCC90	Growth Inhibition Assay		72 h	DMSO	GI50=6.6 ± 1.5 μM	25139387
RPMI-8226	Cell Viability Assay	125/250/500 nM	48h	DMSO	decreases cell viability in a dose-dependent manner	25008202
OPM-2	Cell Viability Assay	125/250/500 nM	48h	DMSO	decreases cell viability in a dose-dependent manner	25008202
RPMI-8226	Apoptosis Assay	125/250/500 nM	48h	DMSO	induces cell apoptosis in a dose-dependent manner	25008202
OPM-2	Apoptosis Assay	125/250/500 nM	48h	DMSO	induces cell apoptosis in a dose-dependent manner	25008202
COG-LL-319	Function Assay	100 nM	1/3/6 h	DMSO	induces caspase-dependent Mcl-1 cleavage	24951472
RS4;11	Function Assay	100 nM	1/3/6 h	DMSO	induces caspase-dependent Mcl-1 cleavage	24951472
FL5.12	Function assay				Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of bovine gelatin, EC50 = 0.008 μM.	17256834
DoHH2	Growth inhibition assay				Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.0083 μM.	17256834
RS11380	Growth inhibition assay				Inhibition of cell growth in human RS11380 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.014 μM.	17256834
FL5.12	Function assay				Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of bovine gelatin, EC50 = 0.03 μM.	17256834
FL5.12	Function assay				Reversal of cytokine withdrawal protection in IL3 dependent Bcl2 overexpressing mouse FL5.12 cells in presence of 3% FBS, EC50 = 0.05 μM.	17256834
DoHH2	Growth inhibition assay				Inhibition of cell growth in human DoHH2 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.13 μM.	17256834
RS11380	Growth inhibition assay				Inhibition of cell growth in human RS11380 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.15 μM.	17256834
SUDHL4	Growth inhibition assay				Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 3% FBS, EC50 = 0.22 μM.	17256834
FL5.12	Function assay				Reversal of cytokine withdrawal protection in IL3 dependent Bcl-xL overexpressing mouse FL5.12 cells in presence of 3% FBS, EC50 = 0.22 μM.	17256834
SUDHL4	Growth inhibition assay				Inhibition of cell growth in human SUDHL4 cells overexpressing Bcl2 in presence of 10% HS, EC50 = 0.85 μM.	17256834
FL5.12	Cytotoxicity assay		24 hrs		Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum, EC50 = 0.0077 μM.	18841882
FL5.12	Cytotoxicity assay		24 hrs		Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum, EC50 = 0.03 μM.	18841882
NCI-H146	Cytotoxicity assay		48 hrs		Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum, EC50 = 0.087 μM.	18841882
CLL	Apoptosis assay				Induction of apoptosis in human CLL cells, EC50 = 0.0045 μM.	20925433
MEF	Cytotoxicity assay		24 hrs		Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum, EC50 = 0.00203 μM.	21366295
MEF	Cytotoxicity assay		24 hrs		Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum, EC50 = 0.051 μM.	21366295
MEF	Cytotoxicity assay		24 hrs		Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum, EC50 = 0.051 μM.	21366295
RS4:11	Antiproliferative assay				Antiproliferative activity against human RS4:11 cells in presence of 10% human serum, EC50 = 0.024 μM.	28926247
MOLT4	Antiproliferative assay				Antiproliferative activity against human MOLT4 cells in presence of 10% human serum, EC50 = 0.622 μM.	28926247
Jurkat	Cytotoxicity assay		48 hrs		Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay, IC50 = 1.38 μM.	19743858
HCT116	Cytotoxicity assay		48 hrs		Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay, IC50 = 4.06 μM.	19743858
SU-8686	Cytotoxicity assay		48 hrs		Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay, IC50 = 4.24 μM.	19743858
H460	Cytotoxicity assay		48 hrs		Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay, IC50 = 8.03 μM.	19743858
Hepa-1c1c7	Cytotoxicity assay		48 hrs		Cytotoxicity against mouse Hepa-1c1c7 cells after 48 hrs by cell titer-blue assay, IC50 = 8.68 μM.	19743858
MCF7	Cytotoxicity assay		48 hrs		Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay, IC50 = 21.26 μM.	19743858
DU145	Cytotoxicity assay		48 hrs		Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay, IC50 = 27.6 μM.	19743858
HCT116	Cytotoxicity assay		72 hrs		Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay, IC50 = 47.7 μM.	22172701
BL21 (DE3)	Function assay		2 hrs		Binding affinity to N-terminus 6X His-tagged human Bcl2 expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, IC50 = 0.002 μM.	22448988
BL21 (DE3)	Function assay		2 hrs		Binding affinity to N-terminus 8X His-tagged human Bcl-xL expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, IC50 = 0.006 μM.	22448988
NCI-H146	Growth inhibition assay		4 days		Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay, IC50 = 0.097 μM.	22448988
NCI-H1417	Growth inhibition assay		4 days		Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay, IC50 = 0.13 μM.	22448988
CCRF-CEM	Cytotoxicity assay		48 hrs		Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 0.74 μM.	22582991
HL60	Cytotoxicity assay		48 hrs		Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 0.76 μM.	22582991
K562	Cytotoxicity assay		48 hrs		Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50 = 34.7 μM.	22582991
NCI-H146	Antiproliferative assay		4 days		Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay, IC50 = 0.037 μM.	22747598
NCI-H1963	Antiproliferative assay		4 days		Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay, IC50 = 0.059 μM.	22747598
NCI-H1417	Antiproliferative assay		4 days		Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay, IC50 = 0.412 μM.	22747598
RS4:11	Apoptosis assay		48 hrs		Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry, IC50 = 0.27 μM.	23314054
K562	Apoptosis assay		48 hrs		Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry, IC50 = 16.4 μM.	23314054
NCI-H1963	Cytotoxicity assay		4 days		Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.054 μM.	23448298
NCI-H187	Cytotoxicity assay		4 days		Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.1377 μM.	23448298
NCI-H1417	Cytotoxicity assay		4 days		Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay, IC50 = 0.1734 μM.	23448298
HL60	Growth inhibition assay		72 hrs		Growth inhibition of human HL60 cells after 72 hrs by MTT assay, IC50 = 0.97 μM.	27712939
MCF7	Growth inhibition assay		72 hrs		Growth inhibition of human MCF7 cells after 72 hrs by MTT assay, IC50 = 25.33 μM.	27712939
U266	Growth inhibition assay		72 hrs		Growth inhibition of human U266 cells after 72 hrs by MTT assay, IC50 = 27.35 μM.	27712939
SKOV3	Growth inhibition assay		72 hrs		Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay, IC50 = 46.59 μM.	27712939
RS4:11	Cytotoxicity assay		24 hrs		Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50 = 0.33 μM.	29453135
Remb1	Cytotoxicity assay		24 hrs		Cytotoxicity against human Remb1 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50 = 1.4 μM.	29453135
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 G196A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.001 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A93V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0014 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 Y195F mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0015 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Wild type Bcl-2-like protein 1 expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0034 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 E129H mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0045 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 E96G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.0058 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142Gdelta136T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.01 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.021 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.058 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 delta136T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.06 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.073 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 R100E mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.16 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 V141A mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.19 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 A142T mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.27 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 L130G mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.29 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 F97V mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.3 μM.	21807512
BL21	Function assay	10 uM	3 hrs		Displacement of BODIPY-Bak conjugated peptide from GST-tagged human Bcl-2-like protein 1 Y101H mutant expressed in Escherichia coli BL21 cells at 10 uM after 3 hrs by fluorescence polarization competition assay, Ki = 0.38 μM.	21807512
BL21 (DE3)	Function assay		2 hrs		Binding affinity to N-terminus 6X His-tagged human Bcl2 expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, Ki = 0.0006 μM.	22448988
BL21 (DE3)	Function assay		2 hrs		Binding affinity to N-terminus 8X His-tagged human Bcl-xL expressed in Escherichia coli BL21 (DE3) cells after 2 hrs by fluorescence polarization assay, Ki = 0.001 μM.	22448988
Toledo	Apoptosis assay				Induction of apoptosis in human Toledo cells, LD50 = 0.06 μM.	24900652
KB	Cytotoxicity assay	0.5 uM			Cytotoxicity in human siRNA-mediated-MCL1-kncok down KB cells overexpressing BCL2 at 0.5 uM	18040043
Eu-Myc	Apoptosis assay	1 uM			Induction of apoptosis in mouse Eu-Myc cells overexpressing BCL2 assessed as inhibition of colony formation at 1 uM	18040043
HeLa	Function assay	1 uM	12 hrs		Induction of Bcl-xL-mediated apoptosis in doxycyclin-stimulated human HeLa cells overexpressing Noxa at 1 uM after 12 hrs by Hoechst staining	22386982
HeLa	Function assay	10 uM	16 hrs		Inhibition of Rluc-Bax/eYFP-Bcl-xL interaction expressed in human HeLa cells at 10 uM after 16 hrs by BRET assay	22425031
MDA-MB-231	Function assay	0.03 to 1 uM	1 hr		Antagonist activity at recombinant Bcl-XL assessed as restoration of BIM BH3-induced Smac protein release in mitochondria isolated from MDA-MB-231 cells at 0.03 to 1 uM after 1 hr by Western blot analysis	22747598
MDA-MB-231	Function assay	0.03 to 1 uM	1 hr		Antagonist activity at recombinant Bcl-XL assessed as restoration of BIM BH3-induced cytochrome c release in mitochondria isolated from MDA-MB-231 cells at 0.03 to 1 uM after 1 hr by Western blot analysis	22747598
BP3	Apoptosis assay	10 uM	24 hrs		Induction of apoptosis in human BP3 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method	23047228
IM9	Apoptosis assay	10 uM	24 hrs		Induction of apoptosis in human IM9 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method	23047228
RS4:11	Apoptosis assay	10 uM	24 hrs		Induction of apoptosis in human RS4:11 cells at 10 uM incubated for 24 hrs by Annexin V and propidium iodide staining based FACS method	23047228
HCT116	Apoptosis assay		48 hrs		Induction of apoptosis in human HCT116 p53+/+ cells after 48 hrs by Annexin V-FITC staining-based flow cytometric method	26982372
DMS53	Apoptosis assay	5 to 10 uM	12 hrs		Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as cytochrome c release at 5 to 10 uM after 12 hrs by immunoblotting method	26982372
DMS53	Function assay	5 to 10 uM	12 hrs		Inhibition of BCl-2/Bim interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method	26982372
DMS53	Apoptosis assay	5 to 10 uM	12 hrs		Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as PARP cleavage at 5 to 10 uM after 12 hrs by immunoblotting method	26982372
DMS53	Apoptosis assay	5 to 10 uM	12 hrs		Induction of apoptosis in human DMS53 cells harboring p53 mutant assessed as caspase-3 cleavage at 5 to 10 uM after 12 hrs by immunoblotting method	26982372
DMS53	Function assay	5 to 10 uM	12 hrs		Inhibition of BCl-2/Bax interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method	26982372
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh30	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
Cliquez pour voir plus de données expérimentales sur les lignées cellulaires

Informations chimiques, stockage et stabilité

Poids moléculaire	813.43	Formule	C₄₂H₄₅ClN₆O₅S₂	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	852808-04-9	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	N/A			Smiles	CN(C)CCC(CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-]

Solubilité

In vitro
Lot:

DMSO : 163 mg/mL (200.38 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 40%PEG300 2 5%Tween80 3 53%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	2.000mg/ml (2.46mM)	Taking the 1 mL working solution as an example, add 20 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 530 μL ddH2O to adjust the volume to 1 mL. . The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Fonctionnalités	First-generation inhibitor of anti-apoptotic Bcl-2 proteins.
Targets/IC₅₀/Ki	Bcl-2 (Cell-free assay) 30.3 nM(EC50) Bcl-xL (Cell-free assay) 78.7 nM(EC50) Bcl-w (Cell-free assay) 197.8 nM(EC50) Bcl-B (Cell-free assay) 1.82 μM(EC50)
In vitro	ABT-737 montre une faible activité envers Bcl-B et aucun effet envers Mcl-1 et BFL-1. Ce composé est sensible aux cellules HL60, KG1 et NB4 avec des IC50 de 50 nM, 80 nM et 80 nM, respectivement. Il induit l'Apoptosis dans les cellules HL60, ce qui est dû à une hétérodimérisation Bcl-2/Bax diminuée et n'a aucun effet sur la distribution du cycle cellulaire. Il induit également la libération de cytochrome c des mitochondries purifiées et favorise les changements conformationnels de Bax qui sont associés à l'Apoptosis. Les cellules résistantes (Hela et MCF-7) peuvent être sensibilisées à ce produit chimique par des approches qui régulent à la baisse, déstabilisent ou inactivent Mcl-1. Il provoque également la libération de cytochrome c dépendante de Bax/BAK uniquement lorsque Mcl-1 a été neutralisé. Ce composé déplace Bim de la poche de liaison BH3 de Bcl-2, permettant à Bim d'activer Bax, d'induire la perméabilisation mitochondriale et d'engager rapidement les cellules de leucémie lymphoïde chronique (LLC) primaires vers la mort. Le knockdown de Mcl-1 avec de l'ARNi sensibilise deux lignées cellulaires de CPSC résistantes H196 et DMS114 en améliorant l'induction de l'Apoptosis. De même, la régulation à la hausse de Noxa sensibilise les cellules H196 à ce produit chimique. Il inhibe la prolifération et induit l'Apoptosis dans de nombreuses lignées cellulaires de CPSC, y compris NCI-H889, NCI-H1963, NCI-H1417, NCI-H146 et etc. Bcl-2 et Noxa peuvent contribuer mécaniquement à la réponse cellulaire à ce produit dans les cellules NCI-H146. Une étude récente montre qu'il induit significativement l'Apoptosis dans les lignées cellulaires T infectées par le HTLV-1 ainsi que dans les cellules ATLL fraîches.
Kinase Assay	Essais de polarisation de fluorescence
Kinase Assay	L'affinité de liaison des protéines de la famille GST-Bcl-2 au domaine BH3 conjugué au FITC de Bim (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) est déterminée. En bref, 100 nM de protéines de fusion de la famille GST-Bcl-2 sont incubées avec des dilutions en série d'ABT-737 dans du PBS pendant 2 min. Ensuite, 20 nM de peptide FITC-Bim BH3 (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) sont ajoutés. La polarisation de fluorescence est mesurée à l'aide d'un système de détection Analyst TM AD Assay après 10 min en utilisant la plaque noire à 96 puits. Ensuite, les IC50 sont déterminées.
In vivo	Dans un modèle de leucémie agressive, ABT-737 supprime la charge leucémique de 53% à 30 mg/kg, avec une survie des souris significativement prolongée. Ce composé n'induit pas d'anomalies significatives dans les numérations sanguines ou les analyses chimiques sériques. Il prolonge la survie des souris receveuses transplantées avec des tumeurs transduites par Bcl-2. Ce produit chimique montre une grande activité antitumorale dans un modèle de souris ATLL à une dose de 100 mg/kg.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/17097560/ [2] https://pubmed.ncbi.nlm.nih.gov/17097561/ [3] https://pubmed.ncbi.nlm.nih.gov/17200714/ [4] https://pubmed.ncbi.nlm.nih.gov/17283153/ [5] https://pubmed.ncbi.nlm.nih.gov/22138435/ [6] https://pubmed.ncbi.nlm.nih.gov/18451169/ [7] https://pubmed.ncbi.nlm.nih.gov/18604177/ [8] https://pubmed.ncbi.nlm.nih.gov/18591385/ [9] https://pubmed.ncbi.nlm.nih.gov/19246337/

Applications

Méthodes	Biomarqueurs	PMID
Western blot	PARP / c-PARP / cleaved caspase 3 Hif-1a γ-H2AX / p-ATM	21393866
Immunofluorescence	cytochrome C Bax Bim AIF p65	26447615
Growth inhibition assay	Cell viability	22311987
ELISA	IL-6 / IL-8	21084274

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

Si vous avez dautres questions, veuillez laisser un message.

Questions fréquemment posées

Question 1:
What is the recommended method for reconstituting it for in vivo animal study?

Réponse :
For oral administration, we suggest the vehicle: 30% Propylene glycol, 5% Tween 80, 65% D5W, at up to 30mg/ml; For injection, it can be dissolved in 2% DMSO/50% PEG 300/5% Tween 80/ddH2O at 2.5 mg/ml.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):