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Sigma-Aldrich

MRP1 Inhibitor II, Reversan

The MRP1 Inhibitor II, Reversan controls the biological activity of MRP1. This small molecule/inhibitor is primarily used for Cell Structure applications.

Synonym(s):

MRP1 Inhibitor II, Reversan, Multidrug Resistance Protein 1 Inhibitor, Reversan

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About This Item

Empirical Formula (Hill Notation):
C26H27N5O2
Molecular Weight:
441.52
UNSPSC Code:
12352200
NACRES:
NA.28

Quality Level

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

pale yellow

solubility

DMSO: 10 mg/mL

shipped in

wet ice

storage temp.

2-8°C

General description

A cell-permeable pyrazolopyrimidine that selectively inhibits MRP1. It is shown to increase the efficacy of vincristine and etopiside by 10- to 15-fold and 7- to 10-fold, respectively, over either of these two MRP1 substrate drugs alone in murine models of neuroblastoma (syngenic and human xenografts). As opposed to the majority of inhibitors of multidrug transporters, it is demonstrated that Reversan was not toxic by itself nor did it increase the toxicity of chemotherapeutic drug exposure in mice. Therefore, Reversan represents a new class of nontoxic MRP1 inhibitor, which may be a useful research tool for the study of neuroblastoma and other MRP1-overexpressing drug-refractory tumors.
A cell-permeable pyrazolopyrimidine that selectively inhibits MRP1. It is shown to increase the efficacy of vincristine and etopiside by 10- to 15-fold and 7- to 10-fold, respectively, over either of these two MRP1 substrate drugs alone in murine models of neuroblastoma (syngenic and human xenografts). As opposed to the majority of inhibitors of multidrug transporters, it is demonstrated that Reversan was not toxic by itself nor did it increase the toxicity of chemotherapeutic drug exposure in mice. Therefore, Reversan represents a new class of nontoxic MRP1 inhibitor, which may be a useful research tool for the study of neuroblastoma and other MRP1-overexpressing drug-refractory tumors.

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Burkhart, C.A., et al. 2009. Cancer Res.69, 6573.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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