Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrates no significant inhibition of non-kinase off-targets.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 336 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,970 | 现货 | ||
50 mg | ¥ 4,580 | 现货 | ||
100 mg | ¥ 6,530 | 现货 | ||
500 mg | ¥ 13,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 788 | 现货 |
产品描述 | Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrates no significant inhibition of non-kinase off-targets. |
体外活性 | Pirtobrutinib potently inhibits both wild-type BTK and BTK C481S-mediated kinase activity with nanomolar potency. Pirtobrutinib strongly inhibits WT BTK (Y223) autophosphorylation with an IC50 of 3.68 nM. Pirtobrutinib inhibits BTK C481S Y223, C481T Y223, and C481R Y223 autophosphorylation with IC50s of 8.45, 7.23, and 11.73 nM, respectively[1]. |
分子量 | 479.43 |
分子式 | C22H21F4N5O3 |
CAS No. | 2101700-15-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (104.29 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 | 2.0858 mL | 10.4291 mL | 20.8581 mL | 52.1453 mL |
5 mM | 0.4172 mL | 2.0858 mL | 4.1716 mL | 10.4291 mL | |
10 mM | 0.2086 mL | 1.0429 mL | 2.0858 mL | 5.2145 mL | |
20 mM | 0.1043 mL | 0.5215 mL | 1.0429 mL | 2.6073 mL | |
50 mM | 0.0417 mL | 0.2086 mL | 0.4172 mL | 1.0429 mL | |
100 mM | 0.0209 mL | 0.1043 mL | 0.2086 mL | 0.5215 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。
Pirtobrutinib 2101700-15-4 Angiogenesis Tyrosine Kinase/Adaptors BTK LOXO 305 inhibit LOXO-305 Btk C81S LOXO305 Bruton tyrosine kinase proliferative Inhibitor mutations autophosphorylation inhibitor