Chemical Name: 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
Biological ActivityABT 737 is a high affinity Bcl-2 family inhibitor (Ki ≤ 1nM for Bcl-XL, Bcl-2 and Bcl-w). BH3 mimetic; triggers Bax/Bak-mediated apoptosis. Exhibits cytotoxicity in lymphoma cell lines overexpressing bcl-2 (EC50 < 1 μM) and multiple myeloma cells (IC50 = 5-15 μM). Induces apoptosis in patient-derived CLL cells. Promotes regression of SCLC tumors in a mouse xenograft model. Synergizes with certain other anticancer agents.
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An inhibitor of Bcl-2 family proteins induces regression of solid tumours.
Oltersdorf et al.
The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized.
van Delft, MF et al.
Cancer Cell., 2006;10:389
ABT-737, an inhibitor of Bcl-2 family proteins, is a potent inducer of apoptosis in multiple myeloma cells.
Kline et al.
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