TW-37是一種有效的BCL-2小分子抑制劑(Ki = 290 nmol/L)，它減弱BCL-2的激活并抑制多個(gè)BCL-2家族成員，包括BCL-XL(Ki = 1110 nmol/L)和MCL-1 (Ki = 260 nmol/L)。它與BCL-2的BCL-2同源結(jié)構(gòu)域3 (BH3)溝結(jié)合，防止促凋亡蛋白(如Bid、Bim和Bad)與BCL-2異二聚化，并隨后允許它們誘導(dǎo)凋亡。最近的研究表明，TW-37能夠抑制多種癌細(xì)胞(如乳腺癌、前列腺癌、淋巴瘤和胰腺癌)的生長(zhǎng)，因?yàn)樗ㄟ^(guò)調(diào)節(jié)幾種重要的細(xì)胞周期相關(guān)基因，包括p27、p57、E2F-1、cdc25A、CDK4、細(xì)胞周期蛋白A、細(xì)胞周期蛋白D1和細(xì)胞周期蛋白e，誘導(dǎo)S期細(xì)胞周期停滯.

產(chǎn)品性質(zhì)：

Cas No.:877877-35-5

別名:N-[4-(2-叔丁基苯磺酰基)苯基]-2,3,4-三羥基-5-(2-異丙基苯基甲基)苯甲酰胺,TW37,TW 37

化學(xué)名: N-[4-(2-tert-butylphenyl)sulfonylphenyl]-2,3,4-trihydroxy-5-[(2-propan-2-ylphenyl)methyl]benzamide

Canonical SMILES: CC(C)C1=CC=CC=C1CC2=C(C(=C(C(=C2)C(=O)NC3=CC=C(C=C3)S(=O)(=O)C4=CC=CC=C4C(C)(C)C)O)O)O

分子式:C33H35NO6S

分子量:573.7

溶解度:≥ 19.75 mg/mL in DMSO, ≥ 3.41 mg/mL in EtOH with ultrasonic and warming

儲(chǔ)存條件；Store at -20°C

注意事項(xiàng)：

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References:

[1].Zhiwei Wang, Asfar Sohail Azmi, Aamir Ahmad, Sanjeev Banerjee, Shaomeng Wang, Fazlul H. Sarkar, and Ramzi M. Mohammad. 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;69:2757-2765

[2].Naoki Ashimori, Benjamin D. Zeitlin, Zhaocheng Zhang, Kristy Warner, IIan M. Turkienicz, Aaron C. Spalding, Theodoros N. Teknos, Shaomeng Wang, and Jacques E. Nor. 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;8:893-903