A multidrug-resistance modulator
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Biochemicals

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Cancer
Multidrug Resistance
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PSC 833

Item No. 20391

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 20 mg/mLDMF:PBS (pH 7.2)(1:3): 0.25 mg/mLDMSO: 3 mg/mLEthanol: 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    Cayman Chemical
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    Product Description

    PSC 833 is a non-immunosuppressant derivative of cyclosporine and potent multidrug-resistance (MDR) modulator.1 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 (Item No. 11764), daunorubicin (Item No. 14159), doxorubicin (Item No. 15007), and etoposide (Item No. 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).2 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.1,3 PSC 833 also prolongs the anti-hyperalgesic effects of intraperitoneally administered pregabalin in a mouse model of cold stress-induced central pain.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Boesch, D., Gavériaux, C., Jachez, B., et al. In vivo circumvention of P-glycoprotein-mediated multidrug resistance of tumor cells with SDZ PSC 833. Cancer Res. 51(16), 4226-4233 (1991).

    2. Shirakawa, K., Takara, K., Tanigawara, Y., et al. Interaction of docetaxel ("Taxotere") with human P-glycoprotein. Jpn. J. Cancer Res. 90(12), 1380-1386 (1999).

    3. Keller, R.P., Altermatt, H.J., Nooter, K., et al. SDZ PSC 833, a non-immunosuppressive cyclosporine: its potency in overcoming P-glycoprotein-mediated multidrug resistance of murine leukemia. Int. J. Cancer 50(4), 593-597 (1992).

    4. Mukae, T., Fujita, W., and Ueda, H. P-glycoprotein inhibitors improve effective dose and time of pregabalin to inhibit intermittent cold stress-induced central pain. J. Pharmacol. Sci. 131(1), 64-67 (2016).