| 分子量(MW): | 573.7 | |
|---|---|---|
| 化学式: | C33H35NO6S | |
| 溶解度: | DMSO ≥115mg/mL Water <1mg/mL Ethanol ≥4mg/mL | |
| 纯度: | >99% | |
| 稳定性: | at -20℃ 2 years | |
| CAS号: | 877877-35-5 |
TW-37 is a Bcl-2 protein family inhibitor with a Ki of 0.29 μM. 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 Ki 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 μM for primary human endothelial cells and averaged 0.3 μM 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 agent treatment. [1][2]
| MEF cells were treated for 24 hours with the Bcl-2 antagonists TW-37at the indicated doses.Acute survival was monitored by propidium iodide uptake assays(red lines).Long term survival(red line) was measured by replacing the drug-containing media with normal media and incubating the cells until visible colonies formed.Clonogenic survival is expressed relative to the numbers of colonies formed following 24 hours incubation in normal media(lacking drugs). | |
| MDB-MA-231 cells were exposed to 30 um cisplatin in the absence or in thepresence of 100 nm TW-37.The cell were stained with Hoechst 33342,MitoTracker Red and Yo-pro-1.
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