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Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

Cetuximab (C225) is a monoclonal antibody that is an inhibitor of human epidermal growth factor receptor (EGFR) (Kd=0.201 nM). Cetuximab has antitumor activity, inhibiting tumor cell proliferation and inducing apoptosis.

Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties.

PF-06459988 is a novel, effective, orally active, irreversible, and selective epidermal growth factor receptor (EGFR) mutant inhibitor. PF-06459988 has high efficiency and high affinity for EGFRs double mutants containing T790M, and has minimal activity against WT EGFR. PF-06459988 makes a candidate drug for the treatment of cancer.

Lapatinib (GW572016) is an inhibitor of ErbB2 and EGFR (IC50=9.2/10.8 nM) with oral activity. Lapatinib has antitumor activity and can be used to treat advanced or metastatic breast cancer with HER2 overexpression.

Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.

Mutated EGFR-IN-1 (Osimertinib analog) is a valuable intermediate in designing inhibitors for mutated EGFR, including L858R EGFR, Exon19 deletion activating mutant, and T790M resistance mutant.

Genistein (NPI 031L) is a naturally occurring soy isoflavone, a multi-targeted tyrosine kinase inhibitor. Genistein has antitumor, antioxidant, and anthelmintic properties, and also produces estrogen-like effects in the body.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Neratinib (HKI-272) (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.

Tucatinib (ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).

Dacomitinib (PF299)(PF299804; PF-00299804) is a highly selective, orally bioavailable small-molecule inhibitor of the HER family of tyrosine kinases with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.

Osimertinib mesylate (AZD-9291 mesylate) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib mesylate has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

Lapatinib Ditosylate (Tykerb ditosylate) is an effective EGFR and ErbB2 inhibitor (IC50: 10.8/9.2 nM for EGFR/ErbB2).

Canertinib (CI-1033) is a pan-erbB tyrosine kinase inhibitor which work against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantly affects tumour metabolism, proliferation and hypoxia as determined by PET.

EGFR ErbB-2 ErbB-4 inhibitor-2 (EGFR ErbB2 Inhibitor) is a cell-permeable compound that inhibits EGFR and c-ErbB2 with IC50 values of 20 nM and 79 nM, respectively.

Tyrphostin B44, (+) enantiomer is an inhibitor of epidermal growth factor receptor (EGFR) kinase with IC50 of 0.86 μM and has less active than the (-) enantiomer.

JCN037 is potent, non-covalent and brain-penetrant inhibitor of EGFR(EGFR, p-wtEGFR and pEGFRvⅢ with IC50 of 2.49 nM, 3.95 nM, 4.48 nM , respectively).

AV-412 (MP412) is an EGFR inhibitor for EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M, and ErbB2, with IC50 values of 0.75, 0.79, 0.5, 2.3, and 19 nM, respectively.

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

AZ7550 hydrochloride (AZ7550 hydrochloride ), an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

Allitinib (AST-1306) (AST-1306) has anti-cancer activity,and it is an irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. [1]