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ABT-737 Bcl-2 remmer

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

Cat.Nr.S1002

ABT-737 is een BH3-mimetische remmer van Bcl-xL, Bcl-2 en Bcl-w met een EC50 van respectievelijk 78,7 nM, 30,3 nM en 197,8 nM in celvrije assays; geen remming waargenomen tegen Mcl-1, Bcl-B of Bfl-1. ABT-737 induceert mitochondriale route Apoptosis en Mitophagy. Fase 2.

Chemische structuur

Moleculair gewicht: 813.43

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Kwaliteitscontrole

Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Overige Bcl-2 Inhibitoren	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

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	813.43	Formule	C₄₂H₄₅ClN₆O₅S₂	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	852808-04-9	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	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-]

Oplosbaarheid

In vitro
Batch:

DMSO : 163 mg/mL (200.38 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Kenmerken	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 vertoont een lage activiteit tegen Bcl-B en geen effecten tegen Mcl-1 en BFL-1. Deze verbinding is gevoelig voor HL60, KG1 en NB4 cellen met een IC50 van respectievelijk 50 nM, 80 nM en 80 nM. Het induceert Apoptosis in HL60 cellen, wat te wijten is aan verminderde Bcl-2/Bax heterodimerisatie en heeft geen effect op de celcyclusdistributie. Het induceert ook cytochroom c afgifte uit gezuiverde mitochondria en bevordert conformationele veranderingen in Bax die geassocieerd zijn met Apoptosis. Resistente cellen (Hela en MCF-7) kunnen gesensibiliseerd worden voor deze chemische stof door benaderingen die Mcl-1 down-reguleren, destabiliseren of inactiveren. Het veroorzaakt ook Bax/BAK-afhankelijke cytochroom c afgifte alleen wanneer Mcl-1 is geneutraliseerd. Deze verbinding verdringt Bim uit de BH3-bindingspocket van Bcl-2, waardoor Bim Bax kan activeren, mitochondriale permeabilisatie kan induceren en de primaire chronische lymfatische leukemie (CLL) cellen snel tot sterfte kan brengen. Knockdown van Mcl-1 met siRNA sensibiliseert twee resistente SCLC-cellijnen H196 en DMS114 ervoor door de inductie van Apoptosis te verbeteren. Evenzo sensibiliseert up-regulatie van Noxa H196-cellen voor deze chemische stof. Het remt de proliferatie en induceert Apoptosis in veel SCLC-cellijnen, waaronder NCI-H889, NCI-H1963, NCI-H1417, NCI-H146 en dergelijke. Bcl-2 en Noxa kunnen mechanistisch bijdragen aan de cellulaire respons erop in NCI-H146-cellen. Een recente studie toont aan dat het significant Apoptosis induceert in HTLV-1 geïnfecteerde T-cellijnen, evenals in verse ATLL-cellen.
Kinase Assay	Fluorescentiepolarisatie-assays
Kinase Assay	De bindingsaffiniteit van GST-Bcl-2-familie-eiwitten aan het FITC-geconjugeerde BH3-domein van Bim (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) wordt bepaald. Kortom, 100 nM GST-Bcl-2-familie-fusie-eiwitten worden gedurende 2 min geïncubeerd met seriële verdunningen van ABT-737 in PBS. Vervolgens wordt 20 nM FITC-Bim BH3-peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) toegevoegd. Fluorescentiepolarisatie wordt gemeten met behulp van een Analyst TM AD Assay Detection System na 10 min met behulp van de 96-well zwarte plaat. Daarna worden de IC50's bepaald.
In vivo	In een agressief leukemiemodel onderdrukt ABT-737 de leukemieziekte met 53% bij 30 mg/kg, met een significant verlengde overleving van muizen. Deze verbinding veroorzaakt geen significante afwijkingen in bloedceltellingen of serumbiochemie. Het verlengt de overleving van ontvanger-muizen die getransplanteerd zijn met Bcl-2-getransduceerde tumoren. Deze chemische stof vertoont een grote antitumoractiviteit in een ATLL-muismodel bij een dosis van 100 mg/kg.
Referenties	[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/

Toepassingen

Methoden	Biomarkers	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

Technische ondersteuning

Gebruiksaanwijzing

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

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Veelgestelde vragen

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

Antwoord:
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.

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