Pirtobrutinib (Synonyms: LOXO-305, LY3527727) |
| Katalog-Nr.GC62515 |
Pirtobrutinib (LOXO-305), ein hochselektiver und nicht-kovalenter BTK-Inhibitor der nÄchsten Generation, hemmt verschiedene BTK-C481-Substitutionsmutationen. Pirtobrutinib verursacht eine Regression von BTK-abhÄngigen Lymphomtumoren in Maus-Xenograft-Modellen. Pirtobrutinib ist auch mehr als 300-fach selektiv fÜr BTK im Vergleich zu 370 anderen getesteten Kinasen und zeigt keine signifikante Hemmung von Nicht-Kinase-Off-Targets bei 1 μM.
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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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