ONT-093

ONT-093 is an orally bioavailable substituted diarylimidazole inhibitor of P-glycoprotein ATPase activity (IC50 = 0.16 µM). It reverses drug resistance to doxorubicin (Cay-15007), vinblastine (Cay-11762), and paclitaxel (Cay-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.Formal Name: 4-[2-[4-[(1E)-3-ethoxy-1-propen-1-yl]phenyl]-4-[4-[(1-methylethyl)amino]phenyl]-1H-imidazol-5-yl]-N-(1-methylethyl)-benzenamine. CAS Number: 216227-54-2. Synonyms: OC 144093. Molecular Formula: C32H38N4O. Formula Weight: 494.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble. lambdamax: 274, 359 nm. SMILES: CCOC/C=C/C1=CC=C(C2=NC(C3=CC=C(NC(C)C)C=C3)=C(C4=CC=C(NC(C)C)C=C4)N2)C=C1. InChi Code: InChI=1S/C32H38N4O/c1-6-37-21-7-8-24-9-11-27(12-10-24)32-35-30(25-13-17-28(18-14-25)33-22(2)3)31(36-32)26-15-19-29(20-16-26)34-23(4)5/h7-20,22-23,33-34H,6,21H2,1-5H3,(H,35,36)/b8-7+. InChi Key: RSJCLODJSVZNQA-BQYQJAHWSA-N.