Pirtobrutinib (LOXO-305) is a highly selective, non-covalent next-generation BTK inhibitor effective against wild-type and C481-mutant BTK (IC50s = 10-100 nM and <10 nM, respectively). It is over 300-fold selective for BTK versus 370 other kinases and does not significantly inhibit non-kinase off-targets at 1 μM. Pirtobrutinib induces regression of BTK-dependent lymphoma tumors in mouse xenograft models and reduces Ki67-positive proliferating cells in MEC-1 chronic lymphocytic leukemia (CLL) models. Reagent grade, for research purpose.
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