Pirtobrutinib

Description: Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 µM, Pirtobrutinib demonstrates no significant inhibition of non-kinase off-targets. Target: BTK. Smiles: COc1ccc(F)cc1C(=O)NCc1ccc(cc1)-c1nn([C@@H](C)C(F)(F)F)c(N)c1C(N)=O. References: 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.