Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,300 | 现货 | ||
5 mg | ¥ 2,900 | 现货 | ||
10 mg | ¥ 4,290 | 现货 | ||
25 mg | ¥ 6,850 | 现货 | ||
50 mg | ¥ 9,270 | 现货 | ||
100 mg | ¥ 12,500 | 现货 | ||
500 mg | ¥ 24,800 | 现货 |
产品描述 | CP 461 (UNII-68OJX9I7DT), a specific PDE2A inhibitor, is a novel pro-apoptotic compound that inhibits cyclic GMP phosphodiesterase but not cyclooxygenase-1 or -2. CP 461 inhibits the growth of a variety of human tumor cell lines in vitro and selectively induces apoptosis in cancer cell lines, but not in normal cells. |
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] |
别名 | OSI 461, UNII-68OJX9I7DT, CP-461, CP461 |
分子量 | 420.91 |
分子式 | C25H22ClFN2O |
CAS No. | 227619-96-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 16.67 mg/mL (39.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3758 mL | 11.879 mL | 23.758 mL | 59.3951 mL |
5 mM | 0.4752 mL | 2.3758 mL | 4.7516 mL | 11.879 mL | |
10 mM | 0.2376 mL | 1.1879 mL | 2.3758 mL | 5.9395 mL | |
20 mM | 0.1188 mL | 0.594 mL | 1.1879 mL | 2.9698 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CP 461 227619-96-7 Apoptosis Metabolism PDE OSI 461 UNII-68OJX9I7DT OSI-461 CP-461 OSI461 CP461 Inhibitor inhibitor inhibit