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Antitumor agent-76

CAS: 2787593-12-6 F: C28H36ClNO10 W: 582.04

Antitumor agent-76 (Compound TP-P1) is an orally active, rapid-release and water-soluble Triptolide (HY-32735) prodrug w
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Bioactivity Antitumor agent-76 (Compound TP-P1) is an orally active, rapid-release and water-soluble Triptolide (HY-32735) prodrug with antitumor activity[1].
Invitro 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[1].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[1].Antitumor agent-76 (30-120 nM; 24 h) shows antiproliferative activities against acute myeloid leukemia (AML) cells without cytotoxicity towards normal cells[1]. Cell Proliferation Assay[1] Cell Line:
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[1].Antitumor agent-76 (100, 300 μg/kg/day; i.g.; 11 days) dose-dependently inhibits tumor growth in mouse MV-4-11 xenograft models[1].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[1].Pharmacokinetic study of Antitumor agent-76 (Compound TP-P1) and triptolide on Sprague Dawley ratsa[1]. Compd
Name Antitumor agent-76
CAS 2787593-12-6
Formula C28H36ClNO10
Molar Mass 582.04
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [1]. Kang D, et al. Discovery of a novel water-soluble, rapid-release triptolide prodrug with improved drug-like properties and high efficacy in human acute myeloid leukemia. Eur J Med Chem. 2022 Sep 5;243:114694.