Chemical Name : ABT737
CAS : 852808-04-9
Synonyms: 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:10 mmol/L in DMSO
Storage:at -20C 2 years
Biologieal
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
Reference
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]