MTX-531

MTX-531 is an EGFR antagonist and PI3K inhibitor. It selectively inhibits EGFR over HER2 and HER4 (IC50s = 14. 2,500, and >10,000 nM, respectively) and PI3Kdelta, PI3Kalpha, and PI3Kgamma over PI3Kbeta (IC50s = 1. 6. 8. and 233 nM, respectively) but also inhibits DNA-dependent protein kinase (DNA-PK, IC50s = 5. nM). MTX-531 also induces gene expression in a reporter assay using HEK293 cells expressing PPARgamma (EC50 = 3. µM). It decreases phosphorylated levels of Akt and 4E-BP1 and induces apoptosis in CAL-33 tongue squamous cell carcinoma cells when used at concentrations ranging from 3 to 10 µM. MTX-531 (100 mg/kg per day) reduces tumor volume and increases survival in a CAL-33 mouse xenograft model.. Solulibility: DMSO: Soluble: = 10 mg/ml: Ethanol: Slightly soluble: 0.1-1 mg/ml.