Manufacturer: Focus Biomolecules
MTX-531 is a first-in-class dual EGFR/pan-PI3K inhibitor (IC50s: EGFR = 14.7 nM; PI3kα = 6.4 nM; PI3Kß = 233 nM; PI3Kγ = 8.3 nM; PI3Kδ = 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.
CAS Number: 2791417-66-6
Manufacturer Part Number/SKU: 10-4802-25mg-EA
Tags: Focus Biomolecules