TW-37/TW37

877877-35-5

编号ABP000129 化学名称TW-37/TW37 英文名称 TW-37/TW37 分子式C33H35NO6S 分子量573.699 纯度 >99%

化学名称 : TW-37/TW37

CAS : 877877-35-5

英文名称: TW-37/TW37

英文同义词: N-[4-[(2-tert-Butylphenyl)sulfonyl]phenyl]-2,3,4-trihydroxy-5-[(2-isopropylphenyl)methyl]benzamide

溶解度:Soluble in DMSO

储存条件:-20C 2 years

生物活性

TW-37 binds to the BH3 binding groove in Bcl-2 protein competing with BH3 peptides derived from Bid, Bim, and Bad proteins. TW-37 binds to Bcl-2 with a K(i) value of 290 nM and also to Bcl-xL and Mcl-1 with high affinities.TW-37 potently inhibits cell growth in PC-3 prostate cancer cells with an IC50 value of 200 nM and effectively induces apoptosis in a dose-dependent manner. TW-37 has an IC50 of 1.1 µmol/L for primary human endothelial cells and averaged 0.3 µmol/L for head and neck cancer cells (OSCC3,UM-SCC-1, and UMSCC-74A). The combination of TW-37 and cisplatin showed enhanced cytotoxic effects for endothelial cells and HNSCC in vitro, compared with single drug treatment.

参考文献

1. Zeitlin BD, Joo E, Dong Z, Warner K, Wang G, Nikolovska-Coleska Z, Wang S, Nör JE. Antiangiogenic effect of TW37, a small-molecule inhibitor of Bcl-2. Cancer Res. 2006 Sep 1;66(17):8698-706. 2. Mohammad RM, Goustin AS, Aboukameel A, Chen B, Banerjee S, Wang G, Nikolovska-Coleska Z, Wang S, Al-Katib A. Preclinical studies of TW-37, a new nonpeptidic small-molecule inhibitor of Bcl-2, in diffuse large cell lymphoma xenograft model reveal drug action on both Bcl-2 and Mcl-1. Clin Cancer Res. 2007 Apr 1;13(7):2226-35. 3. Wang Z, Song W, Aboukameel A, Mohammad M, Wang G, Banerjee S, Kong D, Wang S, Sarkar FH, Mohammad RM. TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and invasion in pancreatic cancer. Int J Cancer. 2008 Aug 15;123(4):958-66. 4. Wang Z, Azmi AS, Ahmad A, Banerjee S, Wang S, Sarkar FH, Mohammad RM. TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and induces apoptosis in pancreatic cancer: involvement of Notch-1 signaling pathway. Cancer Res. 2009 Apr 1;69(7):2757-65. Epub 2009 Mar 24. 5. Ashimori N, Zeitlin BD, Zhang Z, Warner K, Turkienicz IM, Spalding AC, Teknos TN, Wang S, Nör JE. TW-37, a small-molecule inhibitor of Bcl-2, mediates S-phase cell cycle arrest and suppresses head and neck tumor angiogenesis. Mol Cancer Ther. 2009 Apr;8(4):893-903.
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