XR 9051 HCl
Cat. No. 2944
Chemical Name: N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-
Biological ActivityPotent modulator of P-glycoprotein-mediated multidrug resistance (MDR) that inhibits the binding of cytotoxics to P-glycoprotein (EC50 = 134 nM). Reverses resistance to a variety of cytotoxic drugs (including doxorubicin, etoposide and vincristine) in several murine and human P-gp-overexpressing cell lines. Orally active.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Dale et al (1998) Reversal of P-glycoprotein-mediated multidrug resistance by XR9051, a novel diketopiperazine derivative. Br.J.Cancer 78 885. PMID: 9764579.
Mistry et al (1999) In vivo efficacy of XR9051, a potent modulator of P-glycoprotein mediated multidrug resistance. Br.J.Cancer 79 1672. PMID: 10206276.
Martin et al (2000) Communication between multidrug binding sites on P-glycoprotein. Mol.Pharmacol. 58 624. PMID: 10953057.
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Keywords: XR 9051 HCl, supplier, Potent, modulators, P-gp-mediated, MDR, P-glycoprotein, Resistance, Protein, Multidrug, Transporters, XR9051, ABCB1