R&D Systems Inc. Tocris Bioscience Boston Biochem

XR 9051 HCl

Cat. No. 2944

XR 9051 HCl C39H38N4O5.HCl [180422-22-4]

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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

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

M.Wt:
679.2
Formula:
C39H38N4O5.HCl
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
180422-22-4

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

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

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.

If you know of a relevant citation for this product please let us know.

View Related Products by Target

Keywords: XR 9051 HCl, supplier, Potent, modulators, P-gp-mediated, MDR, P-glycoprotein, Resistance, Protein, Multidrug, Transporters, XR9051, ABCB1

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