產(chǎn)品屬性：
產(chǎn)品名稱(chēng) | Pirtobrutinib |
規(guī)格 | 5 mg、10 mg、25 mg、50 mg、100 mg |
貨號(hào) | EY-01Y17554 |
Cas No.: 2101700-15-4
別名: N/A
化學(xué)名: N/A
分子式: C22H21F4N5O3
分子量: 479.43
溶解度: DMSO : 50 mg/mL (104.29 mM; Need ultrasonic)
儲(chǔ)存條件: 4°C, stored under nitrogen
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM[1].Pirtobrutinib potently inhibits both wild-type BTK and BTK C481S-mediated kinase activity with nanomolar potency. Pirtobrutinib 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].[1]. Gomez E B , et al. Loxo-305, a Highly Selective and Non-Covalent Next Generation BTK Inhibitor, Inhibits Diverse BTK C481 Substitution Mutations[J]. Blood, 2019, 134(Supplement_1):4644-4644.
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