Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ALK-IN-12 is a highly potent and orally active inhibitor of anaplastic lymphoma kinase (ALK), demonstrating an exceptional IC50 value of 0.18 nM. Additionally, ALK-IN-12 displays inhibitory activity against insulin-like growth factor 1 receptor (IGF1R) and insulin receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. Notably, its antitumor effects have been observed, making it a promising compound for targeted cancer therapy.
产品描述 | ALK-IN-12 is a highly potent and orally active inhibitor of anaplastic lymphoma kinase (ALK), demonstrating an exceptional IC50 value of 0.18 nM. Additionally, ALK-IN-12 displays inhibitory activity against insulin-like growth factor 1 receptor (IGF1R) and insulin receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. Notably, its antitumor effects have been observed, making it a promising compound for targeted cancer therapy. |
体外活性 | ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC 50 of 28.3 nM[1]. |
体内活性 | ALK-IN-12 (10-50 mg/kg; orally; once daily for 13 consecutive days) shows dose-dependent antitumor activity[1]. ALK-IN-12 (3 mg/kg; i.v.; 6-8 week old female CD rats ) treatment shows AUC 0-∞ , CL, t 1/2 and V ss are 3039 ng?h/mL, 0.91 h?kg, 6.6 hours and 6.12 L/kg, respectively[1]. ALK-IN-12 (10 mg/kg; p.o.; 6-8 week old female CD rats) treatment shows C max , AUC 0-∞ , t max , t 1/2 and F are 3254 ng/mL, 4056 ng?h/mL, 6.0 hours, 12.5 hours and 39%, respectively[1]. Animal Model: Eight- to 10-week old female SCID/beige mice (Karpas-299 xenograft mouse model expressing the NPM-ALK fusion)[1]Dosage: 10-50 mg/kg Administration: Orally; once daily for 13 consecutive days Result: Dose-dependent antitumor activity. Led to tumor stasis (50 mg/kg dose). |
分子量 | 500.97 |
分子式 | C24H30ClN6O2P |
CAS No. | 1197958-53-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
ALK-IN-12 1197958-53-4 ALKIN12 ALK IN 12 Inhibitor inhibitor inhibit