6-[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoicacid]-7-L-valine-cyclosporinA

Name	Valspodar
Synonyms	Psc 833 Valspodar Sdz psc 833 Sdz-psc-833 3'-Keto-bmt(1)-Val(2)-cyclosporin a 6-[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoicacid]-7-L-valine-cyclosporinA Cyclosporin A, 6-((R-(E))-6,7-didehydro-N,4-dimethyl-3-oxo-L-2-aminooctanoic acid)-7-L-valine- 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]
CAS	121584-18-7
EINECS	1312995-182-4

Molecular Formula	C63H111N11O12
Molar Mass	1214.62
Density	1.015±0.06 g/cm3(Predicted)
Melting Point	143-145°C
Boling Point	1290.1±65.0 °C(Predicted)
Specific Rotation(α)	D20 -255.1° (c = 0.5 in CHCl3)
Solubility	Chloroform (Slightly), Methanol (Slightly)
Appearance	powder
Color	white to beige
pKa	12.45±0.70(Predicted)
Storage Condition	-20°C
In vitro study	Valspodar (PSC 833) has no cytotoxicity effects at up to the concentration of 0.75 μg/mL. Valspodar (0.25, 0.5 and 0.75 μg/mL) and DOX-L are added to the DOX resistant cells, and cell kill efficacy of MDR cell type increases significantly when valspodar is administered alongside DOX-L. Valspodar (0.5 and 0.75 μg/mL), in combination with all concentrations of DOX, are most toxic and kill more than 70% of the resistant cells. Pretreatment with PSC833 decreases the IC 50 value of NSC 279836 in MDA-MB-435mdr cells to 0.4±0.02 μM in MDR cells and almost completely reverses the resistance of MDR cells to NSC 279836.
In vivo study	valspodar (10 mg/kg, o.p.) exhibits minimal blood-cell partitioning as reflected in its low mean blood-to-plasma ratio of approximately 0.52. Valspodar displays properties of slow clearance and a large volume of distribution. Valspodar shows properties of low hepatic extraction and wide distribution, similar to that of its structural analogue CsA. Preadministration of PSC833 to mice increases NSC 279836 fluorescent intensity in MDR tumor to 94% of that in the wild-type tumors.

WGK Germany

Last Update：2024-01-02 23:10:35

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CAS: 121584-18-7
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Mobile: 18021002903
QQ: 3008007409

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6-[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoicacid]-7-L-valine-cyclosporinA Request for Quotation