parsaclisib-free-base

Description: Parsaclisib, formerly known as INCB050465, is a novel and potent PI3Kdelta inhibitor which synergizes with PIM protein kinase inhibition to cause tumor regression in a model of DLBCL. INCB050465 inhibits PI3Kdelta with an IC₅₀ of 1 nM at 1 mM ATP, and shows appr 20, 000-fold selectivity for PI3Kalpha, PI3Kbeta, PI3Kgamma and 57 other kinases. INCB050465 displays potent activity with IC50 ranging from 0.2 to 2 nM. In addition, INCB050465 blocks the proliferation of several DLBCL and MCL cell lines in vitro (EC50 < 10 nM) and can slow tumor growth in the Pfeiffer model of DLBCL in vivo. References: Abstract2671: INCB050465, a novel PI3Kdelta inhibitor, synergizes with PIM proteinkinase inhibition to cause tumor regression in a model of DLBCL. CancerResearch. 2015, Aug. 75(15).

Related CAS #: 1995889-48-9 (HCl) 1426698-88-5 (free base)