Synonyms: OBI3424 | TH-3424 | TH3424
Compound class:
Synthetic organic
Comment: OBI-3424 is a prodrug that is converted (activated) by aldo-keto reductase family 1 member C3 (AKR1C3) into an intermediary metabolite that spontaneously hydrolyses to generate a thiotepa-related DNA alkylating (cross-linking) agent [1]. It was designed as a chemotherapeutic agent, and has demonstrated efficacy in preclinical models of T-cell acute lymphoblastic leukemia (T-ALL).
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Bioactivity Comments |
Cytotoxic IC50 of OBI-3424 in H460 lung cancer cells is 4 nM, and it is more potent in cell lines with the highest AKR1C3 expression [1]. |