MI-773 (SAR405838) 是一种口服生物有效的MDM2拮抗剂，Ki为0.88 nM。Phase 1。 应用 SAR405838 是 MI-773 的类似物，具有抗肿瘤活性。它是一种高效、选择性的Mdm2-p53相互作用抑制剂，与 Mdm2 结合的Ki值为 0.88 nM。 Information MI-773 (SAR405838) MI-773 (SAR405838) is an orally available MDM2 antagonist with K i of 0.88 nM. Phase 1. Targets p53 ; MDM2 (Cell-free assay) ; 0.88 nM(Ki) In vitro MI-773 binds to MDM2 with Ki of 0.88 nM. MI-773 potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10 μM), PC-3 (IC50, >10 μM), SW620 (IC50, >10 μM), and HCT-116 (p53 -/- ) (IC50, >20 μM) cells. In vivo In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg,). Cell Research(from reference) Cell lines：SJSA-1, RS4;11, LNCaP, SAOS-2, PC-3, SW620, HCT-116, and HCT-116 (p53 -/- ) cells Concentrations：100 μM Incubation Time：~48 h