S80071
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- 公司名稱 上海源葉生物科技有限公司
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- 產(chǎn)品描述： Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
- 靶點(diǎn)： IC50: 3.4 nM (20S proteasome) Ki: 0.93 nM (20S proteasome)
- 體內(nèi)研究： Ixazomib (MLN2238) shows antitumor activity in the CWR22 xenograft model. The antitumor effects of Ixazomib (MLN2238) dosed at 14 mg/kg i.v. or 7 mg/kg i.v. are compared with Bortezomib dosed at 0.8 mg/kg i.v. or 0.4 mg/kg i.v. on a twice weekly regimen. The high dose for both Ixazomib (MLN2238) and Bortezomib shows similar antitumor activity in this model (T/C=0.36 and 0.44, respectively). However, Ixazomib (MLN2238) (7 mg/kg) shows greater efficacy at a 0.5 MTD dose compared with a 0.5 MTD dose of Bortezomib (0.4 mg/kg; T/C=0.49 compared with T/C=0.79, respectively) Ixazomib (MLN2238) shows time-dependent reversible proteasome inhibition; however, the proteasome dissociation half-life (t1/2) for Ixazomib (MLN2238) is determined to be 18 minutes
- 參考文獻(xiàn)：
1. Kupperman E, et al. Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Res. 2010 Mar 1;70(5):1970-80.
- 溶解度： DMSO : 62.5 mg/mL (173.12 mM; Need ultrasonic)
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 2.77 ml 13.849 ml 27.699 ml 5 mM 0.554 ml 2.77 ml 5.54 ml 10 mM 0.277 ml 1.385 ml 2.77 ml 50 mM 0.055 ml 0.277 ml 0.554 ml
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