XR 9051 HCl
Discontinued Product
Chemical Name: N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-3-[(Z)-[(5Z)-4-methyl-3,6-dioxo-5-(phenylmethylene)piperazinylidene]methyl]benzamide hydrochloride
Purity: ≥98%
Biological Activity
Potent 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Reversal of P-glycoprotein-mediated multidrug resistance by XR9051, a novel diketopiperazine derivative.
Dale et al.
Br.J.Cancer, 1998;78:885 -
In vivo efficacy of XR9051, a potent modulator of P-glycoprotein mediated multidrug resistance.
Mistry et al.
Br.J.Cancer, 1999;79:1672 -
Communication between multidrug binding sites on P-glycoprotein.
Martin et al.
Mol.Pharmacol., 2000;58:624
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