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ABT737

(CAS No:852808-04-9)
ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.
CAS No:852808-04-9
Molecular Weight(MW):813.43
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 852808-04-9
Molecular formula(MF) C42H45ClN6O5S2
Molecular Weight(MW): 813.43
Alias 4-[4-[(4'-Chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]benzamide
Solubility
In vitro DMSO 100 mg/mL (122.93 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% Propylene glycol, 5% Tween 80, 65% D5W 30mg/mL
Biological Activity
Description ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.
Features First-generation inhibitor of anti-apoptotic Bcl-2 proteins.
Targets
Bcl-2 [1]
(Cell-free assay)		 Bcl-xL [1]
(Cell-free assay)		 Bcl-w [1]
(Cell-free assay)		 Bcl-B [1]
(Cell-free assay)		 Bfl-1 [1]
(Cell-free assay)
30.3 nM(EC50) 78.7 nM(EC50) 197.8 nM(EC50) 1.82 μM(EC50) >10 μM(EC50)
In vitro

ABT-737 shows low activity to Bcl-B and no effects to Mcl-1 and BFL-1. ABT-737 is sensitive to HL60, KG1 and NB4 cells with IC50 of 50 nM, 80 nM and 80 nM, respectively. ABT-737 induces apoptosis in HL60 cells, which due to decreased Bcl-2/Bax heterodimerization and has no effect on cell cycle distribution. ABT-737 also induces cytochrome c release from purified mitochondria and promotes conformational changes in Bax that are associated with apoptosis. [1] Resistant cells (Hela and MCF-7) can be sensitized to ABT-737 by approaches that down-regulate, destabilize, or inactivate Mcl-1. ABT-737 also causes Bax/BAK-dependent cytochrome c release only when Mcl-1 has been neutralized. [2] ABT-737 displaces Bim from Bcl2's BH3-binding pocket, allowing Bim to activate Bax, induce mitochondrial permeabilization, and rapidly commit the primary chronic lymphocytic leukemia (CLL) cells to death. [3] Knockdown of Mcl-1 with siRNA sensitizes two resistant SCLC cell lines H196 and DMS114 to ABT-737 by enhancing the induction of apoptosis. Likewise, up-regulation of Noxa sensitizes H196 cells to ABT-737. ABT-737 inhibits proliferation and induces apoptosis in many SCLC cell lines including NCI-H889, NCI-H1963, NCI-H1417, NCI-H146 and etc. Bcl-2 and Noxa may contribute mechanistically to the cellular response to ABT-737 in NCI-H146 cells. [4] A recent study shows that ABT-737 significantly induces apoptosis in HTLV-1 infected T-cell lines as well as in fresh ATLL cells. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description 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

... Click to View More Cell Line Experimental Data
In vivo In aggressive leukemia model, ABT-737 suppresses the leukemia burden by 53% at the 30 mg/kg, with significantly extended survival of mice. ABT-737 does not induce significantly abnormalities in blood cell counts or serum chemistries. [1] ABT-737 prolongs the survival of recipient mice transplanted with Bcl-2-transduced tumors. [2] ABT-737 shows great antitumor activity in an ATLL mouse model at a dose of 100 mg/kg. [5]
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