MLN9708又称伊沙唑米，是第二代小分子蛋白酶体抑制剂。它是一种柠檬酸酯，在暴露于水溶液或血浆时立即水解成其生物活性形式MLN2238。MLN9708是根据与硼替佐米不同的物理化学特征从大量含硼蛋白酶体抑制剂中筛选出来的。MLN9708具有比硼替佐米更短的20S蛋白酶体解离半衰期，这被证明在其改善的组织分布中起重要作用。

产品性质：

Cas No.:1201902-80-8

别名:艾沙佐米柠檬酸盐,MLN-9708, MLN 9708

化学名:[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]boronic acid

Canonical SMILES:B1(OC(=O)CC(O1)(CC(=O)O)C(=O)O)C(CC(C)C)NC(=O)CNC(=O)C2=C(C=CC(=C2)Cl)Cl

分子式:C20H23BCl2N2O9

分子量:517.1

溶解度:≥ 20.85 mg/mL in DMSO, ≥ 4.56 mg/mL in EtOH with ultrasonic and warming

储存条件:Store at -20°C

注意事项：

为了您的安全和健康，请穿实验服并戴一次性手套操作。

References:

[1].Erik Kupperman, Edmund C. Lee, Yueying Cao, Bret Bannerman, Michael Fitzgerald, Allison Berger, Jie Yu, Yu Yang, Paul Hales, Frank Bruzzese, Jane Liu, Jonathan Blank, Khristofer Garcia, Christopher Tsu, Larry Dick, Paul Fleming, Li Yu, Mark Manfredi, Mark Rolfe, and Joe Bolen. Evaluation of the Proteasome Inhibitor MLN9708 in Preclinical Models of Human Cancer. Cancer Res March 1, 2010 70; 1970.

[2].Edmund C. Lee, Michael Fitzgerald, Bret Bannerman, Jill Donelan, Kristen Bano, Jennifer Terkelsen, Daniel P. Bradley, Ozlem Subakan, Matthew D. Silva, Ray Liu, Michael Pickard, Zhi Li, Olga Tayber, Ping Li, Paul Hales, Mary Carsillo, Vishala T. Neppalli, Allison J. Berger, Erik Kupperman, Mark Manfredi, Joseph B. Bolen, Brian Van Ness, Siegfried Janz. Antitumor Activity of the Investigational Proteasome Inhibitor MLN9708 in Mouse Models of B-cell and Plasma Cell Malignancies. Clin Cancer Res December 1, 2011 17; 7313.