XR9051 hydrochloride

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XR9051 hydrochloride is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR).

For research use only. We do not sell to patients.

XR9051 hydrochloride Chemical Structure

CAS No. : 180422-22-4

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Purity & Documentation
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Description

XR9051 hydrochloride is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR)^[1].

In Vitro

XR9051 is able to reverse resistance to a variety of cytotoxic drugs, including doxorubicin, etoposide and vincristine, which are associated with classical MDR^[1].
XR9051 is highly active and gave at least a 15- to 20- fold decrease in the doxorubicin IC₅₀, in the acquired resistance cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

XR9051 (20-40 mg/kg, ip) shows significant modulatory activity in mice bearing MDR human ovarian (2780AD and CH1/DOXr) and SCLC (H69/LX) xenografts^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Balb/c mice (20-25 g)^[2].
Dosage:	I.V.
Administration:	20 mg/kg at various times (5 min to 24 h).
Result:	The area under the concentration time curves (AUC) from time 0-∞ for plasma was 11.9 µg. h mL^-1. The ratio between AUC for tissue:plasma for liver, heart and brain were 79.6, 16.9 and 0.3 respectively.

Animal Model:	MDR 2780AD ovarian carcinoma xenografts^[2].
Dosage:	I.P.
Administration:	20, 30, 40 mg/kg daily with Epirubicin i.v. (10 mg/kg).
Result:	Significantly reduced growth rate of MDR 2780AD ovarian carcinoma xenografts compared with either drug alone.

Molecular Weight

679.20

Formula

C₃₉H₃₉ClN₄O₅

CAS No.

180422-22-4

SMILES

O=C(NC1=CC=C(CCN2CC3=C(C=C(OC)C(OC)=C3)CC2)C=C1)C4=CC=CC(/C=C(C(N(C)/C5=C\C6=CC=CC=C6)=O)\NC5=O)=C4.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. I L Dale , et al. Reversal of P-glycoprotein-mediated multidrug resistance by XR9051, a novel diketopiperazine derivative. Br J Cancer. 1998 Oct;78(7):885-92. [Content Brief]

[2]. P Mistry, et al. In vivo efficacy of XR9051, a potent modulator of P-glycoprotein mediated multidrug resistance. Br J Cancer. 1999 Apr;79(11-12):1672-8. [Content Brief]