Zosuquidar (hydrochloride)

Zosuquidar is a modulator of P-glycoprotein (P-gp, Ki = 59 nM). It restores the sensitivity of P-gp-expressing cancer cells to vinblastine (Cay-11762), doxorubicin (Cay-15007), etoposide (Cay-12092), and paclitaxel (Cay-10461) when used at 0.1 µM. It less potently inhibits cytochrome P450 (CYP) isoforms CYP3A, CYP2D6, and CYP2C9 (Kis = 3.8, 25, and 12 µM, respectively). Zosuquidar does not modulate multidrug resistance-associated protein 1 (MRP-1). Zosuquidar significantly enhances the efficacy of chemotherapeutics in mice implanted with P-gp-expressing tumors. Through its effects on P-gp, zosuquidar enhances the distribution of P-gp substrates through the blood-brain barrier into the brain.Formal Name: (alphaR)-4-[(1aalpha,6alpha,10balpha)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-alpha-[(5-quinolinyloxy)methyl]-1-piperazineethanol, trihydrochloride. CAS Number: 167465-36-3. Synonyms: LY335979, RS 33295-198. Molecular Formula: C32H31F2N3O2 . 3HCl. Formula Weight: 637.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 10 mg/ml, Ethanol:PBS (pH 7.2)(1:2): 0.33 mg/ml. lambdamax: 212, 239, 304 nm. SMILES: FC1(F)[C@@H](C2=C3C=CC=C2)[C@H]1C4=C(C=CC=C4)[C@H]3N(CC5)CCN5C[C@@H](O)COC6=CC=CC7=NC=CC=C76.Cl.Cl.Cl. InChi Code: InChI=1S/C32H31F2N3O2.3ClH/c33-32(34)29-22-7-1-3-9-24(22)31(25-10-4-2-8-23(25)30(29)32)37-17-15-36(16-18-37)19-21(38)20-39-28-13-5-12-27-26(28)11-6-14-35-27,,,/h1-14,21,29-31,38H,15-20H2,3*1H/t21-,29-,30+,31-,,,/m1.../s1. InChi Key: ZPFVQKPWGDRLHL-WITOOOCMSA-N.