化合物CP 461 T31020

Product Introduction
Bioactivity


英文名: CP 461

描述: CP 461 (UNII-68OJX9I7DT) 是一种特异性 PDE2A 抑制剂，是一种新型促凋亡化合物，能抑制环 GMP 磷酸二酯酶，但不能抑制环氧化酶-1 或-2。CP 461 在体外可抑制多种人类肿瘤细胞系的生长，并选择性地诱导癌细胞系而不是正常细胞凋亡。

体内活性: CP-461 inhibits the growth of a broad range of human tumor cell lines in vitro at micromolar concentrations and selectively induces apoptosis in cancer cell lines but not normal cells. Preclinical studies revealed good oral bioavailability and no toxicity in dogs and rats at single doses of up to 500 mg/kg. In a Phase I trial, 21 patients with a range of solid tumors and good performance status received CP-461 p.o. twice daily for 28 consecutive days. Cycles were repeated without a treatment-free interval. CP-461 doses ranged from 100 to 800 mg/day. Therapy was well tolerated overall, and a maximum tolerated dose was not reached. Grade 3 asymptomatic aspartate aminotransferase/alanine aminotransferase elevation in 1 patient treated at 800 mg/day was the only dose-limiting toxicity. No hematologic toxicity was noted. Peak plasma concentrations occurred between 1 and 2 h after dosing, and doses above 200 mg/day exceeded the known in vitro EC(50) (1-2 micro M) for apoptosis in cancer cells. No drug was detectable after 24 h of administration, and the terminal half-life was 6.7 h. The area under the plasma concentration-time curve was dose-proportional from 200 to 800 mg/day. Four patients exhibited disease stability after two cycles of treatment. CP-461 is minimally toxic at doses up to 800 mg/day when administered p.o. on a twice-daily schedule.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 16.67 mg/mL (39.6 mM)


关键字: OSI-461 | OSI461 | CP 461

相关产品: Alpha-Hederin | Chelidonine | Notopterol | K-Ras(G12C) inhibitor 12 | Epibrassinolide | D609 | Samuraciclib hydrochloride | TAS6417 | EI1 | Cucurbitacin IIA

相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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