XR 9051 HCl

Discontinued Product

XR 9051 HCl (Cat. No. 2944) has been withdrawn from sale for commercial reasons.
Cat.No. 2944 - XR 9051 HCl | C39H38N4O5.HCl | CAS No. 180422-22-4
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)
Datasheet
Citations
Reviews
Literature

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
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.

All Tocris products are intended for laboratory research use only.

References

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

Citations for XR 9051 HCl

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