HDS 029 is a potent inhibitor of the ErbB receptor family (IC50 values are 0.3, 0.5 and 1.1 nM for EGFR (ErbB1), ErbB-4 (ErbB4) and Neu (ErbB2) respectively). It inhibits EGF-induced EGFR (erbB1) autophosphorylation in NIH3T3 cells and heregulin-stimulated ErbB autophosphorylation in MDA-MB-453 human breast carcinoma cells (IC50 values are 2.5 and 24 nM respectively).
Klutchko et al (2006) Tyrosine kinase inhibitors. 19. 6-alkynamides of 4-anilinoquinazolines and 4-aniliopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors. J.Med.Chem. 49 1475.
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