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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 (T_1/2=8.64 min) ａnd the clearance rate is high.
Pharmacokinetic study of Antitumor agent-76 (Compound TP-P1) ａnd triptolide on Sprague Dawley rats^a.

^aThe values presented are the mean values from three independent mice.
^bDosed po (oral administration) was administered via oral gavage.

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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