| 产品描述： | 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 |
| 靶点： |
Btk |
| 体外研究： |
Pirtobrutinib 以纳摩尔的效力有效抑制野生型 BTK 和 BTK C481S 介导的激酶活性。Pirtobrutinib 抑制 WT BTK (Y223) 自磷酸化，IC50 为 3.68 nM。Pirtobrutinib 抑制 BTK C481S Y223、C481T Y223 和 C481R Y223 自磷酸化，IC50 分别为 8.45、7.23 和 11.73 nM |
| 体内研究： |
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. |
| 参考文献： |
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. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.086 ml |
10.429 ml |
20.858 ml |
| 5 mM |
0.417 ml |
2.086 ml |
4.172 ml |
| 10 mM |
0.209 ml |
1.043 ml |
2.086 ml |
| 50 mM |
0.042 ml |
0.209 ml |
0.417 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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