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Description: Tariquidar methanesulfonate hydrate (formerly also known as XR9576) is a novel potent and selective noncompetitive inhibitor of P-glycoprotein (P-gp) with Kd of 5.1 nM in CHrB30 cell line, it reverses drug resistance in MDR cell Lines. Tariquidar is currently undergoing research as an adjuvant against multidrug resistance in cancer. Tariquidar non-competitively binds to the p-glycoprotein transporter, thereby inhibiting transmembrane transport of anticancer drugs. Inhibition of transmembrane transport may result in increased intracellular concentrations of an anticancer drug, thereby augmenting its cytotoxicity.
References: Br J Pharmacol. 1999 Sep; 128(2):403-11; Cancer Res. 2001 Jan 15; 61(2):749-58.
Related CAS#: 206873-63-4 (free base); 625375-84-0 (dimesylate); 625375-83-9 (dimesylate hydrate).
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