MLN9708又稱伊沙唑米，是第二代小分子蛋白酶體抑制劑。它是一種檸檬酸酯，在暴露于水溶液或血漿時立即水解成其生物活性形式MLN2238。MLN9708是根據(jù)與硼替佐米不同的物理化學(xué)特征從大量含硼蛋白酶體抑制劑中篩選出來的。MLN9708具有比硼替佐米更短的20S蛋白酶體解離半衰期，這被證明在其改善的組織分布中起重要作用。

產(chǎn)品性質(zhì)：

Cas No.:1201902-80-8

別名:艾沙佐米檸檬酸鹽,MLN-9708, MLN 9708

化學(xué)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

儲存條件:Store at -20°C

注意事項：

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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.