Receptor specificities for selected ErbB tyrosine kinase inhibitors
| Compound | Reversibility of Inhibition | Purified Enzyme Kinase Inhibition IC50 (nmol/L) | Reference(s) | |||||||
|---|---|---|---|---|---|---|---|---|---|---|
| EGFR | HER-2 | ErbB4 | ||||||||
| EGFR specific | ||||||||||
| Gefitinib (Iressa, ZD1839) | Reversible | 27-33 | ≥3,700 | NR | (16) | |||||
| Erlotinib (Tarceva, OSI-774) | Reversible | 2 | >1,000 | NR | (17, 18) | |||||
| EKB-569 | Irreversible | 83 | 1,229 | NR | (19) | |||||
| HER-2 specific | ||||||||||
| CP-724,714 | NR | 4,300 | 8 | NR | (20) | |||||
| TAK165 | NR | NR | NR | NR | (21) | |||||
| Dual or pan-Erb | ||||||||||
| Canertinib (CI-1033) | Irreversible | 0.8 | 19 | 7 | (22) | |||||
| Lapatinib (GW-2016) | Reversible | 11 | 9 | 367 | (23) | |||||
| PKI-166 | Reversible | 1 | 11 | 433 | (24) | |||||
NOTE: NR refers to variables that were not reported in the preclinical reference.