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MI-773

CAS No. : 1303607-07-9

MCE 站：MI-773

产品活性：MI-773 是一种 MDM2-p53 相互作用抑制剂，高亲和力结合到 MDM2，K_i 为 0.88 nM。

研究领域：Apoptosis  |  Metabolic Enzyme/Protease

作用靶点：MDM-2/p53  |  E1/E2/E3 Enzyme

In Vitro: MI-773 potently induces expression of p53 and its downstream targets p21, MDM2, and induces phosphorylation of p53 (serine 392) in low passage primary human ACC cells. Notably, MI-773 induces a dose-dependent increase in the fraction of apoptotic ACC cells and in the fraction of cells in the G1 phase of cell cycle (P<0.05). Consequently, MI-773 causes apoptotic cell death. MI-773 is an advanced synthetic small molecule inhibitor, displays high binding affinity against MDM2 (K_d=8.2 nM).

In Vivo: MI-773 at 10 mg/kg modestly reduces the rate of tumor growth, whereas 100 mg/kg causes significant tumor regression. Control tumors reach an average of 1,000 mm³ at 20 days of treatment, compare to an average volume of 600 mm³ for the 10 mg/kg group and 30 mm³ for the 100 mg/kg group. Kaplan-Meier analysis shows an increase in tumor failure, define as two times increase in tumor volume as compared to pretreatment volume (P=0.044), for vehicle-treated mice when compare to mice treated with 100 mg/kg MI-773.

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