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OBI-3424

CAS No. : 2097713-68-1

產(chǎn)品活性：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.

研究領(lǐng)域：Cell Cycle/DNA Damage

作用靶點：DNA Alkylator/Crosslinker

In Vitro: 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.

In Vivo: 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.

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