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ONT-093 is an orally bioavailable substituted diarylimidazole inhibitor of P-glycoprotein ATPase activity (IC50 = 0.16 µM).1 It reverses drug resistance to doxorubicin (Item No. 15007), vinblastine (Item No. 11762), and paclitaxel (Item No. 10461) in human lymphoma, breast, ovarian, uterine, and colorectal cancer cell lines in vitro (EC50s = 9-38 nM). It is not cytotoxic to 15 normal, non-transformed, or tumor cell lines when used at concentrations up to 100 µM and exhibits weak cytostatic activity (average IC50 = >60 µM). ONT-093 (30 mg/kg) reverses paclitaxel drug resistance in an HCT15 human colon carcinoma mouse xenograft model.
WARNING This product is not for human or veterinary use.
1. Discovery and characterization of OC144-