compound 39

Compound 39 is an irreversible, small-molecule pan-erbB inhibitor characterized by a pyrido[3,4-d]pyrimidine scaffold. It was developed through research at the University of Auckland in collaboration with Pfizer. The compound acts by covalently binding to cysteine residues within the ATP-binding pocket of the erbB family of receptor tyrosine kinases, specifically inhibiting Epidermal Growth Factor Receptor (EGFR/erbB1), HER2 (erbB2), and erbB4. In preclinical enzymatic assays, it demonstrated high potency, with a roughly 10-fold preference for erbB1 over erbB2 and erbB4. In vivo studies showed that Compound 39 achieves significant anti-tumor activity, including regressions in human epidermoid carcinoma (A431), glioblastoma (SF767), and ovarian carcinoma (SKOV3) xenograft models, as well as complete tumor stasis in pancreatic (BXPC3) and non-small-cell lung carcinoma (H125) models.

Other names

pyrido[3,4-d]pyrimidine 39pyrido[3,4-d]pyrimidine analogue 39