pan-PIM inhibitor 17

pan-PIM inhibitor 17 is a potent, selective, orally available inhibitor of Pim kinase with IC50 of 0.8, 5.1 and 1.8 nM for Pim1, 2 and 3, respectively; disaplays broad selectivity in an internal panel of 192 kinases, only eight kinases were inhibited above 50% at 1 uM; demonstrates cellular biomarker pS6 inhibition with EC50 of 27 nM, shows tumor growth inhibition in a KG1 tumor-bearing mouse model.

References 1. Barberis C, et al. Bioorg Med Chem Lett. 2018 Dec 10. pii: S0960-894X(18)30949-1. 2. Barberis C, et al. Bioorg Med Chem Lett. 2017 Oct 15;27(20):4735-4740. 3. Guo Z, et al. Blood. 2014 Sep 11;124(11):1777-89. View Related Products by Target Pim