A BTK inhibitor
Pirtobrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK).1 It inhibits wild-type and mutant BTK (IC50s = 10-100 and <10 nM for wild-type BTK and BTKC481S, respectively). It is selective for BTK over EGFR (IC50 = 1-10 ?M). Pirtobrutinib decreases the number of Ki67-positive cells, a marker of cell proliferation, in MEC-1 chronic lymphocytic leukemia (CLL) mouse xenograft models using MEC-1 cells that express either wild-type BTK or BTKC481S.2
1.Guisot, N.Compounds useful as kinase inhibitors(2017) 2.Aslan, B., Kismali, G., Iles, L.R., et al.Pirtobrutinib inhibits wild-type and mutant Bruton's tyrosine kinase-mediated signaling in chronic lymphocytic leukemiaBlood Cancer J.12(5)80(2022)
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