Table 2.

Receptor specificities for selected ErbB tyrosine kinase inhibitors

CompoundReversibility of InhibitionPurified Enzyme Kinase Inhibition IC50 (nmol/L)
Reference(s)
EGFRHER-2ErbB4
EGFR specific
 Gefitinib (Iressa, ZD1839)Reversible27-33≥3,700NR(16)
 Erlotinib (Tarceva, OSI-774)Reversible2>1,000NR(17, 18)
 EKB-569Irreversible831,229NR(19)
HER-2 specific
 CP-724,714NR4,3008NR(20)
 TAK165NRNRNRNR(21)
Dual or pan-Erb
 Canertinib (CI-1033)Irreversible0.8197(22)
 Lapatinib (GW-2016)Reversible119367(23)
 PKI-166Reversible111433(24)
  • NOTE: NR refers to variables that were not reported in the preclinical reference.