ABT-737

Research use only, not for human use.

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.

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; shows no inhibition against Mcl-1, Bcl-B or Bfl-1; induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway; exhibits single-agent-mechanism-based killing of cells from lymphoma and small-cell lung carcinoma lines, as well as primary patient-derived cells, and in animal models.Ovarian Cancer Phase 2 Clinical.

ABT-737 binds BCL-2, BCL-XL, and BCL-W with high affinity (Ki<1 nM) but binds weakly (Ki>460 nM) to other antiapoptotic BCL-2 family members, including MCL-1 and BFL-1. ABT-737 binds the BH3-binding groove of BCL-XL and BCL-2. ABT-737 (100 nM; 1-72 hours) induces apoptosis and synergizes with chemotherapy in HL-60 cells. ABT-737 (5, 7.5, 10 μM; 72 hours) causes approximately 80% HCT116 cell death. The BAX knockout variant is completely resistant to ABT-737. ABT-737 has no effect on cell cycle distribution. ABT-737 disrupts BCL-2/BAX heterodimerization and induces BAX conformational change in HL-60 leukemic cells. ABT-737 induces a BAX/BAK-dependent impairment of maximal O2 consumption rate in sensitive cells. Stable BCL-2 overexpression in MCF10A cells induces an ABT-737-sensitive primed for death state. ABT-737 induces dose-dependent impairment of maximal O2 consumption rate in B-cell lymphoma cells.

ABT-737 (20, 30 mg/kg/day; i.p.; for 21 days) suppresses the leukemia burden by 48% and 53% at the 20 and 30 mg/kg dose levels, respectively, in four- to six-week-old CB.17 Scid mice with human leukemia KG-1 cells.ABT-737 significantly extends survival of mice in this aggressive leukemia model.

ABT737 | ABT 737

Angiogenesis

Bcl-2

Bcl-2|Bcl-B|Bcl-w|Bcl-xL|Bfl-1

Cancer

Ovarian Cancer

852808-04-9

813.4269

C42H45ClN6O5S2

>98% (HPLC)

10 mM in DMSO

O=C(NS(=O)(C1=CC=C(N[C@H](CCN(C)C)CSC2=CC=CC=C2)C([N+]([O-])=O)=C1)=O)C3=CC=C(N4CCN(CC5=CC=CC=C5C6=CC=C(Cl)C=C6)CC4)C=C3

Benzamide, 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]-

(-20℃)

With Ice Pack

≥ 2 years