AG 825 is a selective inhibitor of ErbB2 and the IC50 values are 0.15 and 19 μM for ErbB2 and ErbB1 respectively.

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.

CL-387785 irreversibly inhibits EGFR with IC50 of 370 pM and shows inhibition of the functional effects of mutations T790M.

TQB3804 is the forth-generation EGFR inhibitor with IC50 values of 7.92nM,0.218nM and 0.16nM for EGFR(WT), EGFR (C797S/T790M/del19) and EGFR (L858R/T790M/C797S), respectively.

Naquotinib is an irreversible mutant EGFR inhibitor with potential antineoplastic activity.

JCN037 is a potent EGFR inhibitor with IC50 values of 2.49 nM, 3.95 nM and 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively. It displayed potent activity against EGFR amplified/mutant patient-derived cell cultures, significant BBB penetration (2:1 brain-to-plasma ratio), and superior efficacy in an EGFR-driven orthotopic glioblastoma xenograft model.

EGFR Inhibitor is a potent, ATP-competitive and highly selective EGFR inhibitor with IC50 values of 21nM, 63nM and 4nM for EGFR, EGFR (L858R) and EGFR (L861Q), respectively. It blocked EGF-induced EGFR autophosphorylation in U-2OS cells at 10µM.

Osimertinib DA is a desacryl analogue of Osimertinib, is an intermediate inhibitor of mutated EGFR, including L858R EGFR, Exonl9 deletion and T790M resistance mutant.

EGFR-IN-5 is an inhibitor of EGFR with IC50 values of 10.4 nM, 1.1 nM, 34 nM and 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively. It could suppress EGFR phosphorylation in a dose-dependent manner in HCC827 cell line and significantly induce the apoptosis of HCC827 cells.

PF-06747775 provides potent EGFR activity against the four common mutants (exon 19 deletion (Del), L858R, and double mutants T790M/L858R and T790M/Del), selectivity over wild-type EGFR, and desirable ADME properties.

AST2818 mesylate is an EGFR inhibitor.

JND3229 is a new highly potent EGFR(C797S) inhibitor with IC50 values of 5.8nM, 30.5nM and 6.8nM for EGFR (L858R/T790M/C797S), EGFR (T790M, L858R) and EGFR, respectively.

AZ5104 is an irreversible inhibitor of EGFR-L858R/T790M, EGFR-L858R, EGFR-L861Q, and EGFR (IC50s of < 1 nM, 6 nM, 1 nM, and 25 nM respectively). AZ5104 is the demethylated metabolite of AZD-9291.

Khellin, a naturally occurring furochromone, is an EGFR inhibitor with an IC50 of 0.15 µM. Khelline has anti-proliferative activity in vitro. Khellin has antispasmodic and coronary vasodilator effects.

Osimertinib Mesylate is a selective inhibitor of mutant EGFR with IC50s of 12 nM and 1 nM for L858R and L858R/T790M in enzyme assay respectively.

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.

Avitinib maleate, the maleate salt form of avitinib, selectively inhibits EGFR L858R/T790M mutant with IC50 of 7.68 nM. It used as antineoplastic drug candidate.

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.