ABT737

852808-04-9

编号ABP000128 化学名称ABT737 英文名称 ABT737 分子式C42H45ClN6O5S2 分子量813.427 纯度 99%

化学名称 : ABT737

CAS : 852808-04-9

英文名称: ABT737

英文同义词: 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

溶解度:10 mmol/L in DMSO

储存条件:at -20C 2 years

生物活性

A selective inhibitor of BCL-2, in small cell lung cancer. ABT-737 induced dramatic regressions in tumors derived from some SCLC cell lines. In vitro, peripheral blood CLL cells are extremely sensitive to ABT-737 (EC50 ~7 nM).

The Bcl-2 antagonist ABT-737 targets Bcl-2/Bcl-xL ,ABT-737 induces Bax conformational change but fails to activate Bak or trigger Bax translocation. Coadministration of roscovitine and ABT-737 untethers Bak from Mcl-1 and Bcl-xL, respectively, triggering Bak activation and Bax translocation

参考文献

1. A novel Bcl-2/Bcl-X(L)/Bcl-w inhibitor ABT-737 as therapy in multiple myeloma.Chauhan D, Oncogene. 2007 Apr 5;26(16):2374-80. Epub 2006 Oct

2. BH3 Mimetic ABT-737 and a Proteasome Inhibitor Synergistically Kill Melanomas through Noxa-Dependent Apoptosis. Miller LA J. Invest. Dermatol. (2008) [Epub ahead of print]

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