S07-2010 is a pan-aldo-keto reductase 1C (AKR1C) inhibitor (IC50s for AKR1C isoforms: 1C1 = 470 nM, 1C2 = 730 nM, 1C3 = 190 nM, 1C4 = 360 nM). Dysregulated AKR1C3 expression (and overexpression of all AKR1C isoforms in general) is related to resistance to radio- and chemotherapy in various tumor types and is associated with development of and poor prognosis in many cancers. S07-2010 displayed cytotoxicity to doxorubicin-resistant MCF-7 cells (IC50 = 127.5 µM) and cisplatin-resistant A549 cells (IC50 = 5.51 µM). Combination treatment of chemotherapeutic agents and S07-2010 showed synergistic effects in drug-resistant cell lines.
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