Valspodar

Valspodar
  • CAS No.:121584-18-7
Other grades of this product :
Valspodar 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:121584-18-7
MF:C63H111N11O12
MW:1214.62
EINECS:1312995-182-4
Product Categories:Intermediates & Fine Chemicals;Peptides;Pharmaceuticals
Mol File:121584-18-7.mol
Valspodar Chemical Properties
Melting point 143-145°C
Boiling point 1290.1±65.0 °C(Predicted)
alpha D20 -255.1° (c = 0.5 in CHCl3)
density 1.015±0.06 g/cm3(Predicted)
storage temp. -20°C
solubility Chloroform (Slightly), Methanol (Slightly)
pka12.45±0.70(Predicted)
form powder
color white to beige
Safety Information
WGK Germany 3
MSDS Information
Valspodar Usage And Synthesis
DescriptionPSC 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 PropertiesWhite Solid
UsesValspodar/ PSC-833 has been used as a ABCB1 (P-glycoprotein) inhibitor.
UsesAntineoplastic adjunct (chemosensitizer).
Brand nameAmdray (Novartis).
Biochem/physiol ActionsValspodar 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.
Valspodar Preparation Products And Raw materials

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