产品
编 号：F615097
分子式：C39H39ClN4O5
分子量：679.2
分子式：C39H39ClN4O5
分子量：679.2
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CAS No: 180422-22-4
产品详情
生物活性：
XR9051 hydrochloride is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR).
体内研究：
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.Animal Model:Female Balb/c mice (20-25 g).
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.
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.
体外研究：
XR9051 is able to reverse resistance to a variety of cytotoxic drugs, including doxorubicin, etoposide and vincristine, which are associated with classical MDR.XR9051 is highly active and gave at least a 15- to 20- fold decrease in the doxorubicin IC50, in the acquired resistance cell lines.
XR9051 hydrochloride is an orally active and specific modulator of P-glycoprotein-mediated multidrug resistance (MDR).
体内研究：
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.Animal Model:Female Balb/c mice (20-25 g).
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.
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.
体外研究：
XR9051 is able to reverse resistance to a variety of cytotoxic drugs, including doxorubicin, etoposide and vincristine, which are associated with classical MDR.XR9051 is highly active and gave at least a 15- to 20- fold decrease in the doxorubicin IC50, in the acquired resistance cell lines.
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