Pirtobrutinib (Synonyms: LOXO-305, LY3527727) |
| Catalog No.GC62515 |
Pirtobrutinib(LOXO-305)는 고도로 선택적이고 비공유적인 차세대 BTK 억제제로 다양한 BTK C481 치환 돌연변이를 억제합니다. 피르토브루티닙은 마우스 이종이식 모델에서 BTK 의존성 림프종 종양의 퇴행을 유발합니다. 피르토브루티닙은 또한 테스트된 370개의 다른 키나제에 비해 BTK에 대해 300배 이상 선택적이며 1μM에서 비-키나제 오프타겟의 유의한 억제를 나타내지 않습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2101700-15-4
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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