PIK-75 HCl

Description: PIK-75 HCl, the hydrochloride salt of PIK-75, is a novel, potent, selective and imidazopyridine-based p110alpha inhibitor with potential anticancer activity and with IC50 of 5.8 nM, which is 200-fold more potent than p110beta. It also potently inhibits DNA-PK with an IC50 of 2 nM in cell-free assays. PIK-75 was developed as part of a PI 3-kinase drug discovery program and is able to attenuate insulin stimulation of Akt/PKB in a range of cell types at 100 nM. PIK-75 has been reported to block growth of a range of cell lines with an IC50 value in the region of 50 nM. In vivo studies showed that PIK-75 (at 50 mg/kg) inhibited the growth of HeLa cell xenografts in mice models. In acute myeloid leukemia (AML) cells, PIK-75 targeted the p110alpha isoform of PI3K, which led to a loss of connection between Bcl-xL and Bak.

References: Mol Pharmacol. 2011 Oct; 80(4):657-64; Blood. 2013 Aug 1; 122(5):738-48.

Related CAS: 372196-67-3 (free base) 372196-77-5 (HCl)