XR 9051 HCl

Discontinued Product

Unfortunately 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 No. 2944) has been withdrawn from sale for commercial reasons.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
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.

Preparing Stock Solutions

The following data is based on the product molecular weight 679.2. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.47 mL 7.36 mL 14.72 mL
5 mM 0.29 mL 1.47 mL 2.94 mL
10 mM 0.15 mL 0.74 mL 1.47 mL
50 mM 0.03 mL 0.15 mL 0.29 mL

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Product Datasheets

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References

References are publications that support the products' biological activity.

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, Multidrug, Transporters, Tocris Bioscience

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Programmed Cell Death

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

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