MTX-531 is a first-in-class dual EGFR/pan-PI3K inhibitor (IC50s: EGFR = 14.7 nM, PI3kalpha = 6.4 nM, PI3Kß = 233 nM, PI3Kgamma = 8.3 nM, PI3Kdelta = 1.1 nM, mTOR = 105 nM, DNA-PK = 5.4 nM). MTX-531 displayed exquisite selectivity for EGFR and PI3K family members (against >400 protein/lipid kinases). It displayed efficacy in the treatment of head and neck squamous cell carcinomas and in combination with RAS inhibitors in BRAF-mutant and KRAS-mutant colorectal and pancreatic cancers. Additionally, it did not produce a hyperglycemic response that is typical for PI3K inhibitors. An interesting new chemical tool for cancer research that targets two key resistance drivers.
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