Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZ12601011 is a highly potent and selective inhibitor of the TGFBR1 kinase, administered orally. It displays an IC50 of 18 nM and a Kd of 2.9 nM. By selectively targeting ALK4, TGFBR1, and ALK7, AZ12601011 effectively inhibits the phosphorylation of SMAD2. Additionally, it has been shown to hinder the growth and metastasis of mammary tumors [1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 9,850 | 10-14周 | ||
50 mg | ¥ 12,800 | 10-14周 | ||
100 mg | ¥ 17,900 | 10-14周 |
产品描述 | AZ12601011 is a highly potent and selective inhibitor of the TGFBR1 kinase, administered orally. It displays an IC50 of 18 nM and a Kd of 2.9 nM. By selectively targeting ALK4, TGFBR1, and ALK7, AZ12601011 effectively inhibits the phosphorylation of SMAD2. Additionally, it has been shown to hinder the growth and metastasis of mammary tumors [1]. |
靶点活性 | ALK4:, TGFBR1:18 nM, TGFBR1:2.9 nM (kd) |
体外活性 | AZ12601011 (0.01-10 μM; for 20 minutes) entirely inhibits Phosphorylation of SMAD2 [1]. AZ12601011 (0.01 μM-10 μM) inhibits the activity of ALK4, ALK7 and TGFBR1 [1]. AZ12601011 inhibits 4T1 cells growth in vitro (IC 50 =0.4μM) [1]. Western Blot Analysis [1] Cell Line: NIH3T3, HaCaT, C2C12, T47D cells Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM Incubation Time: 20 minutes Result: Completely inhibited Phosphorylation of SMAD2. |
体内活性 | AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and migration in vivo [1]. Animal Model: Female BALB/c mice at greater than 18g with tumour [1] Dosage: 50mg/kg Administration: Oral gavage; twice daily; for 25 days Result: Inhibited both tumour growth and metastasis in vivo. |
分子量 | 313.36 |
分子式 | C19H15N5 |
CAS No. | 2748337-86-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5 mg/mL (15.96 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1912 mL | 15.9561 mL | 31.9122 mL | 79.7804 mL |
5 mM | 0.6382 mL | 3.1912 mL | 6.3824 mL | 15.9561 mL | |
10 mM | 0.3191 mL | 1.5956 mL | 3.1912 mL | 7.978 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。
AZ12601011 2748337-86-0 Angiogenesis Tyrosine Kinase/Adaptors ALK AZ-12601011 AZ 12601011 Inhibitor inhibitor inhibit