Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CD532 是一种高效的 Aurora A 激酶抑制剂,IC50 值为 45 nM。CD532 可阻断 Aurora A 激酶活性,驱动 MYCN 降解,可以直接与 AURKA 相互作用并诱导整体构象转变。CD532 可用于研究癌症。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 266 | 现货 | ||
5 mg | ¥ 622 | 现货 | ||
10 mg | ¥ 997 | 现货 | ||
25 mg | ¥ 1,830 | 现货 | ||
50 mg | ¥ 2,720 | 现货 |
产品描述 | CD532 is A highly potent Aurora A kinase inhibitor with an IC50 value of 45 nM. CD532 can block Aurora A kinase activity, drive MYCN degradation, and can directly interact with AURKA and induce global conformational transformation. CD532 can be used to study cancer. |
靶点活性 | Aurora A:45 nM, Kelly:146.7 nM(EC50), SK-N-BE cells:223.2 nM(EC50) |
体外活性 |
In MYCN-amplified neuroblastoma cell lines SK-N-BE(2) and Kelly, CD532 (1-10000 nM; 72 h) exhibits cytotoxicity with EC50s of 223.2 nM and 146.7 nM, respectively[1]. In SK-N-BE(2) cells, CD532 (0.1-1 μM; 24 h) causes a dose-dependent loss of MYCN protein[1]. Furthermore, CD532 (1 μM; 6 h) prevents S-phase entry in SK-N-BE(2) cells[1]. |
体内活性 |
In mice with subcutaneous sonic hedgehog (SHH)-subtype medulloblastoma, CD532 (25 mg/kg; i.p. twice weekly for 3 weeks) decreases the tumor volume and increases survival[1]. In MYCN-amplified neuroblastoma xenografts, CD532 (60 mg/kg; i.p. for 2 days) reduces the level of MYCN protein[1]. CD532 (20 mg/kg; i.p.) in mice exhibits a serum half-life of ~1.5 hours and an AUC0-24 of 27 μM•h[1]. |
分子量 | 522.52 |
分子式 | C26H25F3N8O |
CAS No. | 1639009-81-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 200 mg/mL (382.76 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 | 1.9138 mL | 9.569 mL | 19.138 mL | 47.8451 mL |
5 mM | 0.3828 mL | 1.9138 mL | 3.8276 mL | 9.569 mL | |
10 mM | 0.1914 mL | 0.9569 mL | 1.9138 mL | 4.7845 mL | |
20 mM | 0.0957 mL | 0.4785 mL | 0.9569 mL | 2.3923 mL | |
50 mM | 0.0383 mL | 0.1914 mL | 0.3828 mL | 0.9569 mL | |
100 mM | 0.0191 mL | 0.0957 mL | 0.1914 mL | 0.4785 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。
CD532 1639009-81-6 Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase 1 [4 ({4 [(5 cyclopentyl 1H pyrazol 3 yl)imino] 1,4 dihydropyrimidin 2 yl}amino)phenyl] 3 [3 (trifluoromethyl)phenyl]urea CD-532 CD 532 1[4({4[(5cyclopentyl1Hpyrazol3yl)imino]1,4dihydropyrimidin2yl}amino)phenyl]3[3(trifluoromethyl)phenyl]urea Inhibitor inhibitor inhibit