ABT-737是一种新型有效的B细胞淋巴瘤2 (BCL-2)家族蛋白抑制剂，该家族蛋白对细胞存活至关重要，并在许多肿瘤细胞中过表达，对BCL-XL、BCL-2和BCL-w具有高亲和力，但对同源性较低的蛋白如BCL-B、MCL-1和A1没有亲和力。ABT-737在体外和体内均显示出抗淋巴瘤和小细胞肺癌的单一药物活性以及显著的抗骨髓瘤活性。在最近的研究中，ABT-737有效地杀死了急性髓性白血病原始细胞、祖细胞和干细胞，而正常造血细胞完好无损。BCL-2/BAX复合物的破坏和BAK依赖性但BIM非依赖性的内在凋亡途径的激活也可以被ABT-737诱导。

产品性质：

Cas No.:852808-04-9

别名:ABT 737, ABT737

化学名: 4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide

Canonical SMILES: CN(C)CCC(CSC1=CC=CC=C1)NC2=C(C=C(C=C2)S(=O)(=O)NC(=O)C3=CC=C(C=C3)N4CCN(CC4)CC5=CC=CC=C5C6=CC=C(C=C6)Cl)[N+](=O)[O-]

分子式:C42H45ClN6O5S2

分子量:813.43

溶解度:≥ 40.67mg/mL in DMSO

储存条件:Store at -20°C

注意事项：

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References:

[1].Marina Konopleva, Rooha Contractor, Twee Tsao, Ismael Samudio, Peter P. Ruvolo, Shinichi Kitada, Xingming Deng, Dayong Zhai, Yue-Xi Shi, Thomas Sneed, Monique Verhaegen, Maria Soengas, Vivian R. Ruvolo, Teresa McQueen, Wendy D. Schober, Julie C. Watt, Tilahun Jiffar, Xiaoyang Ling, Frank C. Marini, David Harris, Martin Dietrich, Zeev Estrov, James McCubrey, W. Stratford May, John C. Reed, and Michael Andreeff. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell 2006: 10; 375-388

[2].Suzanne Trudel, A. Keith Stewart, Zhihua Li, Yanjun Shu, Sheng-Ben Liang, Young Trieu, Donna Reece, Josh Paterson, Dingyan Wang, and Xiao-Yan Wen. The Bcl-2 family protein inhibitor,ABT-737, has substantial antimyeloma activity and shows synergistic effect with dexamethasone and melphalan. Clin Cancer Res 2007; 13 (2) 621-629