Name | 3-[(5-benzylidene-4-methyl-3,6-dioxopiperazin-2-ylidene)methyl]-N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]benzamide,hydrochloride |
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Synonyms | xr 9051 hcl |
Description | XR9051 hydrochloride is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR)[1]. |
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Related Catalog | |
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]. |
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]. 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. |
References |
Molecular Formula | C39H39ClN4O5 |
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Molecular Weight | 679.20 |
Exact Mass | 678.26100 |
PSA | 105.66000 |
LogP | 4.41440 |