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Antitumor agent-76
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Antitumor agent-76
CAS No. : 2787593-12-6
MCE 站:Antitumor agent-76
产品活性:Antitumor agent-76 (Compound TP-P1) 是一种具有口服活性的、快速释放、水溶性的 Triptolide (HY-32735) 前药,具有抗癌活性。
研究领域:Apoptosis
作用靶点:Apoptosis
In Vitro: 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.
In Vivo: 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.
Compd | dosageb (mg/kg) | AUC(0-t) (h ng/ml) | Tmax (h) | VZ/F (L/kg) | CLZ/F (L/h/kg) | Cmax (μg/L) |
Antitumor agent-76 | 1.6 | 60.46 | 0.50 | 37831.99 | 24563.25 | 23.53 |