Tetrahydropyrido[4,3-d]pyrimidine was found, by in vitro cytotoxic and enzymatic assays, to inhibit both ATX and EGFR with anticancer and antifibrotic activity superior to gefitinib, an EGFR inhibitor clinically used for the treatment of lung, breast and other cancers with overactive EGFR signaling. The gene discussed is ENPP2; the disease is cancer.