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Merck
CN

SBPSC

PSC833 - Specific MDR1/P-gp Inhibitor

Synonym(s):

Valspodar, 6-[(2S,4R,6E)-4-Methyl-2-(methylamino)-3-oxo-6-octenoic acid]cyclosporin D, Amdray, PSC833, [3′-Desoxy-3′-oxo-MeBmt]1-[Val]2-cyclosporin

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About This Item

Empirical Formula (Hill Notation):
C63H111N11O12
CAS Number:
121584-18-7
Molecular Weight:
1214.62
UNSPSC Code:
12352200
MDL number:
MFCD00907207

Key Documents

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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)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

InChI key

YJDYDFNKCBANTM-QCWCSKBGSA-N

form

powder

color

white

shipped in

wet ice

storage temp.

−20°C

Biochem/physiol Actions

Valspodar is a nonimmunosuppressive cyclosporin analog and potent P-glycoprotein (MDR1) inhibitor.
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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
SLBN8270V
SLBM8671V
PSCA533
SLBN8271V

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H L Tai
Current opinion in molecular therapeutics, 2(4), 459-467 (2001-03-16)
Valspodar (PSC-833) is a derivative of cyclosporin but devoid of the immunosuppressive and nephrotoxic properties seen in cyclosporin A. It exhibited high affinity binding to Mdr1 P-glycoprotein (P-gp) and demonstrated multidrug resistance-reversing activity superior to cyclosporin A and verapamil both
D Berg et al.
Oncology nursing forum, 26(4), 711-720 (1999-05-25)
To review the mechanisms of multidrug resistance (MDR) in human cancer and the clinical use of MDR modulators to overcome or reverse P-glycoprotein (P-gp)-mediated MDR. Current literature, ongoing clinical trials, and clinical experience. Agents, such as valspodar, that block the
Elias Georges et al.
Biochemical pharmacology, 90(2), 107-114 (2014-05-14)
DPPE, a tamoxifen derivative with antihistamine activity, was previously shown to potentiate the toxicity of chemotherapeutic drugs. Recently, a Phase III clinical study using doxorubicin with DPPE demonstrated significant increase in the overall survival of breast cancer patients. In this

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