产品
编 号：F756006
分子式：C28H36ClNO10
分子量：582.04
分子式：C28H36ClNO10
分子量：582.04
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CAS No: 2787593-12-6
产品详情
生物活性：
Antitumor agent-76 (Compound TP-P1) is an orally active, rapid-release and water-soluble Triptolide (HY-32735) proagent with antitumor activity.
体内研究：
Antitumor agent-76 (Compound TP-P1) (0-1.2 mg/kg; i.p.; daily for 28 days) inhibits tumor cell growth, proliferation and induces tumor cell apoptosis in mouse THP-1 and MV-4-11 xenografts models.Antitumor agent-76 (100, 300 μg/kg/day; i.g.; 11 days) dose-dependently inhibits tumor growth in mouse MV-4-11 xenograft models.Antitumor agent-76 is easily hydrolyzed in liver microsomes due to the high content of esterase in liver. The half-life is short (T1/2=8.64 min) and the clearance rate is high.Pharmacokinetic study of Antitumor agent-76 (Compound TP-P1) and triptolide on Sprague Dawley ratsa.Compddosageb(mg/kg) AUC(0-t) (h ng/ml) Tmax(h) VZ/F(L/kg) CLZ/F(L/h/kg) Cmax(μg/L)
Antitumor agent-761.660.460.5037831.9924563.2523.53
aThe values presented are the mean values from three independent mice. bDosed po (oral administration) was administered via oral gavage.Animal Model:Male BALB/c Nude mice, THP-1 xenograft and MV-4-11 xenograft
Dosage:0.1, 0.3, 0.6, 1.2 mg/kg for THP-1 xenograft, 25, 50, 100 μg/kg for MV-4-11 xenograft
Administration:Intraperitoneal administration, daily for 28 days
Result:Significantly and dose-dependently inhibited the tumor growth in THP-1 xenografts, with an excellent tumor growth inhibitory rate (TGI) of 93.87% at the dosage of 100 μg/kg. Inhibited cell proliferation and induced cell apoptosis in tumor tissues. Also showed excellent antitumor activity in MV-4-11 xenograft models (25 μg/kg with a TGI of 54.3%), and the tumors achieved complete regression on day 12 at the dosage of 100 μg/kg.
Animal Model:Sprague Dawley rats
Dosage:1.6 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:Exhibited an acceptable pharmacokinetic property.
体外研究：
Antitumor agent-76 (Compound TP-P1) shows good stability in aqueous solution, and the aqueous solubility (6.13 mg/mL in water) improved significantly compared to Triptolide.Antitumor agent-76 (50 μg/mL) can be rapidly and completely converted into Triptolide within 30 min in rat plasma and within 45 min in human plasma. The concentration of Antitumor agent-76 has no significant effect on conversion rate.Antitumor agent-76 (30-120 nM; 24 h) shows antiproliferative activities against acute myeloid leukemia (AML) cells without cytotoxicity towards normal cells.
Antitumor agent-76 (Compound TP-P1) is an orally active, rapid-release and water-soluble Triptolide (HY-32735) proagent with antitumor activity.
体内研究：
Antitumor agent-76 (Compound TP-P1) (0-1.2 mg/kg; i.p.; daily for 28 days) inhibits tumor cell growth, proliferation and induces tumor cell apoptosis in mouse THP-1 and MV-4-11 xenografts models.Antitumor agent-76 (100, 300 μg/kg/day; i.g.; 11 days) dose-dependently inhibits tumor growth in mouse MV-4-11 xenograft models.Antitumor agent-76 is easily hydrolyzed in liver microsomes due to the high content of esterase in liver. The half-life is short (T1/2=8.64 min) and the clearance rate is high.Pharmacokinetic study of Antitumor agent-76 (Compound TP-P1) and triptolide on Sprague Dawley ratsa.Compddosageb(mg/kg) AUC(0-t) (h ng/ml) Tmax(h) VZ/F(L/kg) CLZ/F(L/h/kg) Cmax(μg/L)
Antitumor agent-761.660.460.5037831.9924563.2523.53
aThe values presented are the mean values from three independent mice. bDosed po (oral administration) was administered via oral gavage.Animal Model:Male BALB/c Nude mice, THP-1 xenograft and MV-4-11 xenograft
Dosage:0.1, 0.3, 0.6, 1.2 mg/kg for THP-1 xenograft, 25, 50, 100 μg/kg for MV-4-11 xenograft
Administration:Intraperitoneal administration, daily for 28 days
Result:Significantly and dose-dependently inhibited the tumor growth in THP-1 xenografts, with an excellent tumor growth inhibitory rate (TGI) of 93.87% at the dosage of 100 μg/kg. Inhibited cell proliferation and induced cell apoptosis in tumor tissues. Also showed excellent antitumor activity in MV-4-11 xenograft models (25 μg/kg with a TGI of 54.3%), and the tumors achieved complete regression on day 12 at the dosage of 100 μg/kg.
Animal Model:Sprague Dawley rats
Dosage:1.6 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:Exhibited an acceptable pharmacokinetic property.
体外研究：
Antitumor agent-76 (Compound TP-P1) shows good stability in aqueous solution, and the aqueous solubility (6.13 mg/mL in water) improved significantly compared to Triptolide.Antitumor agent-76 (50 μg/mL) can be rapidly and completely converted into Triptolide within 30 min in rat plasma and within 45 min in human plasma. The concentration of Antitumor agent-76 has no significant effect on conversion rate.Antitumor agent-76 (30-120 nM; 24 h) shows antiproliferative activities against acute myeloid leukemia (AML) cells without cytotoxicity towards normal cells.
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