EGFR/ErbB-2/ErbB-4 inhibitor-3

• CAT Number: I010597
• CAS Number: 881001-19-0
• Molecular Formula: C17H11ClFN5O
• Molecular Weight: 355.75
• Purity: ≥95%
• Synonyms: N-[4-(3-chloro-4-fluoroanilino)pyrido[3,4-d]pyrimidin-6-yl]but-2-ynamide
• InChI: InChI=1S/C17H11ClFN5O/c1-2-3-16(25)24-15-7-11-14(8-20-15)21-9-22-17(11)23-10-4-5-13(19)12(18)6-10/h4-9H,1H3,(H,20,24,25)(H,21,22,23)
• InChIKey: DLPSDPPZXRJQOY-UHFFFAOYSA-N
• SMILES: CC#CC(=O)NC1=NC=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl

EGFR/ErbB-2/ErbB-4 inhibitor-3 (compound 29) is a potent tyrosine kinase inhibitor with IC50s of 0.3, 1.1, 0.5, 2.5, 24 nM for erbB1, erbB2, erbB4, EGF, HER, respectively[1]. EGFR/ErbB-2/ErbB-4 inhibitor-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Reference

[1]. Klutchko SR, et al. Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors. J Med Chem. 2006 Feb 23;49(4):1475-85.
 [Content Brief]