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Submit ReviewXR 9051 HCl
Description: Potent modulator of P-gp-mediated MDR
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% (HPLC)
Biological Activity for XR 9051 HCl
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 for XR 9051 HCl
| M. Wt | 679.2 |
| Formula | C39H38N4O5.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 180422-22-4 |
| Smiles | O=C(C3=CC=CC(/C=C5\NC(/C(N(C)C5=O)=C/C4=CC=CC=C4)=O)=C3)NC(C=C2)=CC=C2CCN1CC(C=C(OC)C(OC)=C6)=C6CC1.Cl |
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.
Product Datasheets for XR 9051 HCl
References for XR 9051 HCl
References are publications that support the biological activity of the product.
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, XR 9051 HCl supplier, Potent, modulators, P-gp-mediated, MDR, P-glycoprotein, Resistance, Protein, Multidrug, Transporters, XR9051, ABCB1, 2944, Tocris Bioscience
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