AG-537

A dimeric tyrphostin EGFR inhibitor (IC50 = 0.4 µM), selective for EGFR over the Bcr-Abl fusion proteins p210 and p185 and wild-type c-Abl (IC50s = 44, >100, and >100 µM, respectively, for the human proteins), inhibits EGFR autophosphorylation (IC50 = 3.3 µM), inhibits EGF-dependent proliferation of HER-14 fibroblasts (IC50 = 3 µM), an inhibitor of T. brucei REL1 (IC50 = 0.25 µM) and M. tuberculosis PptT (EC50 = 5.9 µM in a BpsA activation assay). SMILES: OC(C=C1/C=C(C#N)/C(NCCCNC(/C(C#N)=C/C2=CC(O)=C(C=C2)O)=O)=O)=C(C=C1)O. InChi Code: InChI=1S/C23H20N4O6/c24-12-16(8-14-2-4-18(28)20(30)10-14)22(32)26-6-1-7-27-23(33)17(13-25)9-15-3-5-19(29)21(31)11-15/h2-5,8-11,28-31H,1,6-7H2,(H,26,32)(H,27,33)/b16-8+,17-9+. InChi Key: ZHOKHSGWBNPFQU-GONBZBRSSA-N