CAS NO: | 2101700-15-4 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generationBTKinhibitor, inhibits diverseBTKC481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective forBTKversus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM[1]. | ||||||||||||||||
体外研究 (In Vitro) | Pirtobrutinib potently inhibits both wild-type BTK and BTK C481S-mediated kinase activity with nanomolar potency. Pirtobrutinib inhibits WT BTK (Y223) autophosphorylation with an IC50of 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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 479.43 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C22H21F4N5O3 | ||||||||||||||||
CAS 号 | 2101700-15-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 50 mg/mL(104.29 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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