ABT-737是一種新型有效的B細(xì)胞淋巴瘤2 (BCL-2)家族蛋白抑制劑，該家族蛋白對細(xì)胞存活至關(guān)重要，并在許多腫瘤細(xì)胞中過表達(dá)，對BCL-XL、BCL-2和BCL-w具有高親和力，但對同源性較低的蛋白如BCL-B、MCL-1和A1沒有親和力。ABT-737在體外和體內(nèi)均顯示出抗淋巴瘤和小細(xì)胞肺癌的單一藥物活性以及顯著的抗骨髓瘤活性。在最近的研究中，ABT-737有效地殺死了急性髓性白血病原始細(xì)胞、祖細(xì)胞和干細(xì)胞，而正常造血細(xì)胞完好無損。BCL-2/BAX復(fù)合物的破壞和BAK依賴性但BIM非依賴性的內(nèi)在凋亡途徑的激活也可以被ABT-737誘導(dǎo)。

產(chǎn)品性質(zhì)：

Cas No.:852808-04-9

別名:ABT 737, ABT737

化學(xué)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

儲存條件:Store at -20°C

注意事項(xiàng)：

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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