XR9051 hydrochloride
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.
- CAS No.: 180422-22-4
- Formula: C39H39ClN4O5
- Molecular Weight:679.20
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/c mice (20-25 g)[2].
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Dosage:I.V.
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Administration:20 mg/kg at various times (5 min to 24 h).
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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.
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Animal Model:MDR 2780AD ovarian carcinoma xenografts[2].
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Dosage:I.P.
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Administration:20, 30, 40 mg/kg daily with Epirubicin i.v. (10 mg/kg).
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Result:Significantly reduced growth rate of MDR 2780AD ovarian carcinoma xenografts compared with either drug alone.
Chemical Information
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CAS No. 180422-22-4
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Molecular Weight 679.20
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Formula C39H39ClN4O5
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XR9051 hydrochloride Related Classifications
HY-13776A Related Classifications
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