SHP099 is a potent (IC50 = 71 nM) and selective allosteric inhibitor of SHP2. SHP2 is a non-receptor tyrosine phosphatase that regulates cell survival and proliferation through activating the RAS-ERK pathway. It also mediates programmed cell death 1 (PD-1) and T-lymphocyte attenuator (BTLA) immune checkpoint pathways. Treatment with SHP099, in combination with ceritinib, halts growth of ALK-inhibitor resistant non-small-cell lung cancer cells.3 Thus, reduction of SHP2 activity is a potential important cancer therapy target. It showed no activity against a panel of 21 other human phosphatases and 66 kinases.
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