Erlotinib is an EGFR inhibitor with IC50 of 2 nM, > 1000-fold more sensitive for EGFR than human c-Src or v-Abl.

Gefitinibis an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively, and interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells.

Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.

Afatinib E-isomer is an irreversible inhibitor of dual EGFR and HER2 that shows obvious activitives of EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM respectively.

Saracatinib is Src inhibitor with IC50 of 2.7 nM.

Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.

Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2 and EGFR, respectively.

Canertinib is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4.

AG-490 is a broad-spectrum inhibitor that has several targets including EGFR (IC50 = 2 μM), ErbB2 (IC50 = 13.5 μM), STAT3 and JAK2.

Dacomitinib is a potent, orally available, irreversible tyrosine kinase HER 1 (EGFR), HER2 and HER4 inhibitor with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively.

WZ4002 is an irreversible inhibitor of mutant EGFR (L858R) and EGFR (T790M) with IC50 of 2 nM and 8 nM respectively.

AZD8931 is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM respectively.

CUDC-101 inhibits HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM and 15.7 nM, respectively.

PD153035 is EGFR inhibitor with Ki and IC50 of 5.2 pM and 29 pM and could rapidly suppress autophosphorylation of EGFR.

Pelitinib irreversiblly inhibits EGFR with IC50 of 38.5 nM.

OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).

WZ3146 is a mutant-selective irreversible inhibitor of EGFR (L858R) and EGFR (E746_A750) with IC50 of 2 nM and 2 nM and does not inhibit ERBB2 phosphorylation (T798I).

AST-1306 p-toluenesulfonic acid is an irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.

CO-1686 functions as an irreversible and mutant-selective inhibitor of EGFRL858R/T790M and EGFRWT with Ki of 21.5 nM and 303.3 nM respectively.

Varlitinib is a selective and potent ErbB1 (EGFR) and ErbB2 (HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively.