OBI-3424 (Synonyms: TH-3424) |
Katalog-Nr.GC62501 |
OBI-3424 (TH-3424) ist ein Prodrug, das selektiv von AKR1C3 (Aldo-Keto-Reduktase 1C3) in ein wirksames DNA-alkylierendes Mittel umgewandelt wird. OBI-3424 kann in der Forschung zu hepatozellulÄrem Karzinom, kastrationsresistentem Prostatakrebs und akuter lymphoblastischer LeukÄmie (ALL) eingesetzt werden.
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Cas No.: 2097713-68-1
Sample solution is provided at 25 µL, 10mM.
OBI-3424 (TH-3424) is a prodrug 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[1].
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[1].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[1].
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[1].
[1]. Kathryn Evans, et al. OBI-3424, a Novel AKR1C3-Activated Prodrug, Exhibits Potent Efficacy against Preclinical Models of T-ALL. Clin Cancer Res. 2019 Jul 15;25(14):4493-4503.
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