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编 号:F150603
分子式:C30H34Cl2FN5O4
分子量:618.53
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1mg
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5mg
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10mg
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生物活性:
Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.

体内研究:
Milademetan (DS-3032b, 50 mg/kg, oral gavage) delays tumor growth and improves survival in mice xenografted with neuroblastoma cells with functional TP53.Animal Model:SH-SY5Y xenograft tumors in nude mice.
Dosage:50 mg/kg.
Administration:Oral gavage for 30 consecutive days with an alternating schedule of 4 days of daily treatment with oral gavages followed by 2 days without treatment (4+2).
Result:Survival in the mouse cohort was significantly prolonged.Reduced neuroblastoma xenograft tumor growth by activating TP53 signaling.

体外研究:
Milademetan (DS-3032) can stabilize TP53 and selectively induce CDKNA1, BAX and MDM2 expression in neuroblastoma cells with wild-type TP53.Milademetan (DS-3032b) treatment enhances TP53 target gene expression and induces G1 cell cycle arrest, senescence and apoptosis.Milademetan (DS-3032b, 0-2000 nM) treatment selectively inhibits viability, proliferation and migration of neuroblastoma cells with wildtype TP53 independently of MYCN status.
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