IQS-019 mesylate

A novel, potent inhibitor of most upstream tyrosine kinases in BCR signaling pathway, inhibits BCR kinases Lyn, Syk and Btk with IC50 of 0.15 uM, 1.6 uM and 2.1 uM, respectively; inhibits at least 20% of the kinase activity at 0.1 uM) and an almost complete kinase inactivation at the 10 uM in a set of 17 TK/TKLs; impaires cell proliferation, reduces CXCL12-dependent cell migration, and induces caspase-dependent apoptosis; shows improved efficacy in vitro and in vivo compared to ibrutinib.

References 1. Balsas P, et al. J Hematol Oncol. 2017 Mar 31;10(1):80. 2. Puig de la Bellacasa R, et al. Eur J Med Chem. 2014 Oct 30;86:664-75. View Related Products by Target BTK