产品
编 号:F748958
分子式:C21H25N4O6P
分子量:460.42
产品类型
结构图
CAS No: 2097713-68-1
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产品详情
生物活性:
OBI-3424 (TH-3424) is a proagent that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research.
体内研究:
OBI-3424 (0.5-2.5 mg/kg; i.p.; once weekly; for 3 weeks) treatment induces regressions in PDXs mice and results in prolongation of mouse event-free survival.Animal Model:Female NSG mice (20-25 g) bearing patient-derived xenografts (PDX)
Dosage:0.5 mg/kg, 1 mg/kg, 2.5 mg/kg
Administration:Intraperitoneal injection; once weekly; for 3 weeks
Result:Resulted in prolongation of mouse event-free survival.
体外研究:
OBI-3424 exerts potent cytotoxicity against the H460 lung cancer cell line (IC50 of 4.0 nM). OBI-3424 exhibits potent cytotoxicity, in particular against cell lines derived from T-ALL with high AKR1C3 expression, with IC50 values in the low nM range.OBI-3424 also exerts potent cell killing against ALL PDXs, and the median IC50 values were 60.3 nM for B-ALL, 9.7 nM for T-ALL and 31.5 nM for ETP-ALL.