121584-18-7

Basic information

• Product Name: Valspodar
• Synonyms: Valspodar;3'-Keto-bmt(1)-Val(2)-cyclosporin a;Cyclosporin A, 6-((R-(E))-6,7-didehydro-N,4-dimethyl-3-oxo-L-2-aminooctanoic acid)-7-L-valine-;Psc 833;Sdz psc 833;Sdz-psc-833;Cyclo[[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoyl]-L-valyl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl-L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl];6-[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoicacid]-7-L-valine-cyclosporinA
• CAS NO: 121584-18-7
• Molecular Formula: C36H70N4O5
• Molecular Weight: 638.9648
• EINECS: 1312995-182-4
• Product Categories: Intermediates & Fine Chemicals;Peptides;Pharmaceuticals
• Mol File: 121584-18-7.mol
• Article Data: 0

Chemical Properties

• Boiling Point: 1290.1°Cat760mmHg
• Flash Point: 734°C
• Appearance: white to beige/
• Density: 1.015g/cm³
• Vapor Pressure: 0mmHg at 25°C
• Refractive Index: 1.466
• Storage Temp.: Store at -20°C
• Solubility: Chloroform (Slightly), Methanol (Slightly)
• PKA: 12.45±0.70(Predicted)
• CAS DataBase Reference: Valspodar(CAS DataBase Reference)
• NIST Chemistry Reference: Valspodar(121584-18-7)
• EPA Substance Registry System: Valspodar(121584-18-7)

Safety Data

• WGK Germany: 3
• Hazardous Substances Data: 121584-18-7(Hazardous Substances Data)

Usage

Description

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 , daunorubicin , doxorubicin , and etoposide , 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.

Chemical Properties

White Solid

Uses

Different sources of media describe the Uses of 121584-18-7 differently. You can refer to the following data:
1. Valspodar/ PSC-833 has been used as a ABCB1 (P-glycoprotein) inhibitor.
2. Antineoplastic adjunct (chemosensitizer).

Brand name

Amdray (Novartis).

Biochem/physiol Actions

Valspodar is a nonimmunosuppressive cyclosporin analog and potent P-glycoprotein (MDR1) inhibitor. Valspodar reverses multidrug resistance (MDR) by inhibiting cellular drug efflux mediated by P-glycoprotein.

InChI:InChI=1/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)51(40(14)15)63(86)74(52)25/h26-27,34-47,49-52H,28-33H2,1-25H3,(H,64,78)(H,65,77)(H,66,79)(H,67,80)/b27-26+/t41-,42+,43-,44+,45+,46+,47+,49+,50+,51+,52+/m1/s1