475730

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

Properties

• Quality Level: 100
• 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

Description

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable