HM30181

HM30181 is an inhibitor of P-glycoprotein (P-gp), also known as multidrug resistance protein 1 (MDR1, IC50 = 0.63 nM). It is selective for P-gp over breast cancer resistance protein (BCRP, IC50 = 3,700 nM), as well as multidrug resistance-associated protein 1 (MRP1), MRP2, and MRP3 at 100 µM. It inhibits transepithelial basal-to-apical transport of paclitaxel in MDCK monolayers overexpressing P-gp (IC50 = 35.4 nM). HM30181 inhibits tumor growth and induces tumor regression in an HT-29 mouse xenograft model when administered at doses of 10 and 20 mg/kg, respectively, in combination with paclitaxel (Cay-10461).Formal Name: N-[2-[2-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-2H-tetrazol-5-yl]-4,5-dimethoxyphenyl]-4-oxo-4H-1-benzopyran-2-carboxamide. CAS Number: 849675-66-7. Synonyms: Encequidar. Molecular Formula: C38H36N6O7. Formula Weight: 688.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml. SMILES: COC(C=C1C2=NN(C3=CC=C(CCN4CC(C=C(OC)C(OC)=C5)=C5CC4)C=C3)N=N2)=C(C=C1NC(C6=CC(C7=C(O6)C=CC=C7)=O)=O)OC. InChi Code: InChI=1S/C38H36N6O7/c1-47-32-17-24-14-16-43(22-25(24)18-33(32)48-2)15-13-23-9-11-26(12-10-23)44-41-37(40-42-44)28-19-34(49-3)35(50-4)20-29(28)39-38(46)36-21-30(45)27-7-5-6-8-31(27)51-36/h5-12,17-21H,13-16,22H2,1-4H3,(H,39,46). InChi Key: AHJUHHDDCJQACA-UHFFFAOYSA-N.