Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CP-609754 是高效的、可逆的法尼基转移酶抑制剂,对重组人 H-Ras 和重组 K-Ras 法尼基化的 IC50分别为 0.57 ng/mL 和 46 ng/mL。CP-609754有潜在的抗癌作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 690 | 现货 | ||
5 mg | ¥ 1,630 | 现货 | ||
10 mg | ¥ 2,660 | 现货 | ||
25 mg | ¥ 4,530 | 现货 | ||
50 mg | ¥ 6,230 | 现货 | ||
100 mg | ¥ 8,160 | 现货 | ||
500 mg | ¥ 16,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,730 | 现货 |
产品描述 | CP-609754 shows selective inhibition of farnesyltransferase. |
靶点活性 | Farnesylation:1.72 ng/mL |
体外活性 | CP-609754 inhibits farnesylation (IC50 = 1.72 ng/mL) of mutant H-Ras in 3T3 H-ras (61L)-transfected cell lines. CP-609754 selectively inhibits farnesylation of both H- and K-Ras proteins in 3T3 transfectants. CP-609754 is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI. CP-609754 interacts with the farnesyltransferase-farnesyl PPI complex and competes for the binding of the Ras protein[1]. |
体内活性 | CP-609754 has in vivo antitumor activity against 3T3 H-ras (61L) tumors. With twice daily oral dosing of CP-609754, tumor regression is achieved with a dose of 100 mg/kg; the ED50 for tumor growth inhibition is 28 mg/kg. With continuous i.p. infusion of CP-609754, tumor growth is inhibited by >50%, and tumor farnesyltransferase activity inhibited by >30% in mice in which the plasma concentration of CP-609754 is maintained above 118 ng/mL[1]. |
分子量 | 479.96 |
分子式 | C29H22ClN3O2 |
CAS No. | 1190094-64-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (208.35 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0835 mL | 10.4175 mL | 20.8351 mL | 52.0877 mL |
5 mM | 0.4167 mL | 2.0835 mL | 4.167 mL | 10.4175 mL | |
10 mM | 0.2084 mL | 1.0418 mL | 2.0835 mL | 5.2088 mL | |
20 mM | 0.1042 mL | 0.5209 mL | 1.0418 mL | 2.6044 mL | |
50 mM | 0.0417 mL | 0.2084 mL | 0.4167 mL | 1.0418 mL | |
100 mM | 0.0208 mL | 0.1042 mL | 0.2084 mL | 0.5209 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-609754 1190094-64-4 Metabolism Transferase Malignant farnesylation Farnesyltransferase Tumor Inhibitor LNK-754 CP 609754 H-Ras Ftase OSI 754 Farnesyl Transferase LNK 754 OSI-754 inhibit OSI754 LNK754 K-Ras Advanced CP609754 inhibitor