纯度:>98% by HPLC;NMR (Conforms)
分子式:C22H20ClN5O2S
分子量:453.95
溶剂:DMSO (>50 mg/ml)
性状:White solid
存储:-20°C
Activity (short version):Dual EGFR/PI3K inhibitor
Function / Pharmacology:MTX-531 is a first-in-class dual EGFR/pan-PI3K inhibitor (IC50s: EGFR = 14.7 nM; PI3kα = 6.4 nM; PI3K? = 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.