MTX-211

MTX-211 is a dual inhibitor of PI3Kalpha and EGFR (IC50s = <100 nM for both). It reduces viability of 5637, EJ, and UM-UC-3 bladder cancer cells (IC50s = 1.075, 1.514, and 2.189 µM, respectively), an effect that can be partially inhibited by glutathione (GSH). MTX-211 also induces apoptosis, increases the levels of the Nrf2 binding protein Keap1, and reduces the levels of Nrf2 and GSH in 5637 and EJ cells. It reduces tumor growth in a 5637 mouse xenograft model when administered at a dose of 10 mg/kg.. SMILES: O=S(NC1=C(Cl)N=CC(C2=CC=C3N=CN=C(C3=C2)NC4=CC=C(C(Cl)=C4)F)=C1)(C)=O. InChi Code: InChI=1S/C20H14Cl2FN5O2S/c1-31(29,30)28-18-7-12(9-24-19(18)22)11-2-5-17-14(6-11)20(26-10-25-17)27-13-3-4-16(23)15(21)8-13/h2-10,28H,1H3,(H,25,26,27). InChi Key: GUYKCXXNIKKSBC-UHFFFAOYSA-N