ON 146040 is the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways; inhibits PI3K / isoforms with IC50 of 14/20 nM.
ON 146040 was highly potent in killing hematologic tumor cells with IC50 values in the 150 to 1,000 nM range. In biochemical testing, ON 146040 inhibited PI3K / isoforms (IC50 14 and 20 nM, respectively) without having a major effect on / isoforms (IC50 3 and 1 M, respectively). ON 146040 was also found to inhibit Abl1 and several mutant versions of this kinase (IC50 < 150 nM), although the compound was not found to be active against the T315I mutant. Following treatment with ON 146040, STAT3 and STAT5 phosphorylation were down-regulated in leukemia and myeloma cells.
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