PSC 833

PSC 833 is a non-immunosuppressant derivative of cyclosporine and potent multidrug-resistance (MDR) modulator. It restores sensitivity of MDR-P388 murine leukemia cells to cytostatic agents when used at concentrations of 70, 33, 45, 34, and 26 nM in combination with colchicine, vincristine (Cay-11764), daunorubicin (Cay-14159), doxorubicin (Cay-15007), and etoposide (Cay-12092), respectively. PSC 833 inhibits basal-to-apical transport and increases apical-to-basal transport of [14C]docetaxel in LLC-GA5-COLO150 cells that overexpress human P-glycoprotein (P-gp). In vivo, PSC 833 increases survival time in MDR-P388 tumor-bearing mice and in an MDR-L1210 leukemia mouse xenograft model when administered in combination with doxorubicin. PSC 833 also prolongs the anti-hyperalgesic effects of intraperitoneally administered pregabalin in a mouse model of cold stress-induced central pain.Formal Name: 6-[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoic acid]-7-L-valine-cyclosporin A. CAS Number: 121584-18-7. Synonyms: Valspodar. Molecular Formula: C63H111N11O12. Formula Weight: 1214.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/mL, DMF:PBS (pH 7.2)(1:3): 0.25 mg/mL, DMSO: 3 mg/mL, Ethanol: 14 mg/mL. SMILES: C[C@H](C/C=C/C)C([C@@H](C(N[C@H](C(N(CC(N(C)[C@H](C(N[C@@H](C(C)C)C(N(C)[C@H]1CC(C)C)=O)=O)CC(C)C)=O)C)=O)C(C)C)=O)N(C([C@H](C(C)C)N(C([C@@H](N(C([C@H](CC(C)C)N(C([C@H](NC([C@@H](NC1=O)C)=O)C)=O)C)=O)C)CC(C)C)=O)C)=O)C)=O. InChi Code: InChI=1S/C63H111N11O12/c1-26-27-28-41(16)53(76)52-57(80)67-49(38(10)11)61(84)68(19)33-48(75)69(20)44(29-34(2)3)56(79)66-50(39(12)13)62(85)70(21)45(30-35(4)5)55(78)64-42(17)54(77)65-43(18)58(81)71(22)46(31-36(6)7)59(82)72(23)47(32-37(8)9)60(83)73(24)5. InChi Key: YJDYDFNKCBANTM-QCWCSKBGSA-N.