ARRY-380 analog is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold selective for HER2 versus EGFR.

Canertinib 2HCl, an irreversible quinazoline-based HER family tyrosine kinase inhibitor, inhibits EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM respectively. Phase II.

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.

Irbinitinib is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold selective for HER2 versus EGFR.

TAK-788 is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations, including exon 20 insertions. It is in a phase 1/2 open-label, multicenter study.

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.

Poziotinib is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.

Afatinib dimaleate is an irreversible inhibitor of EGFR and HER2, the IC50s for EGFR (wt), EGFR (L858R), EGFR (L858R/T790M) and HER2 are 0.5 nM, 0.4 nM, 10 nM and 14 nM respectively.

Mubritinib is a potent and selective inhibitor of HER2/ErbB2 with IC50 of 6 nM with no inhibition on EGFR, FGFR, PDGFR, and etc.

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

AV-412 is an inhibitor of EGFR (IC50 = 0.5-2 nM), ErbB2 (IC50=19 nM), Abl receptor (IC50 = 41nM), mutant EGFR-L858R (IC50=0.51 nM) and EGFR-T790M (IC50=0.79 nM). It also inhibits autophosphorylation of EGFR and ErbB2 with IC50s of 43 nM and 282 nM, respectively.

TAK-285 is a dual HER2 and EGFR (HER1) inhibitor with IC50 of 17 nM and 23 nM, > 10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.

Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.

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

CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, > 640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc.

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

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

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