SHP099 (SHP-099) is a potent, selective, allosteric and orally bioavailable protein tyrosine phosphatase SHP2 inhibitor with IC50 of 71 nM.
SHP099 exhibits excellent phosphatase selectivity profiling over a panel of 21 human phosphatases (including SHP1) and a panel of 66 serine-threonine and tyrosine kinase.
SHP099 inhibits p-ERK with an IC50 of ~0.25 uM in SHP2- dependent MDA-MB-468 and KYSE520 cells, suppresses RAS–ERK signalling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells in vitro.
SHP099 is efficacious in mouse tumour xenograft models.
