EGFR/ErbB-2 inhibitor-1 is a selective ErbB2/HER2 inhibitor that effectively blocks ErbB2 and HER2 signaling.

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.

Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4).

TAS6417 is an EGFR inhibitor and is an efficacious drug candidate for patients with NSCLC (IC50: ranging from 1.1-8.0 nM).

Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.

Butein (2’,3,4,4’-tetrahydroxy Chalcone), a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit EGFR.

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.

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

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.

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. BI-4020 exhibits activity agains 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 exhibits high kinome selectivity and good DMPK properties.

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.

Genistein (NPI 031L) is an isoflavonoid derived from soy products. It inhibits protein-tyrosine kinase and topoisomerase-II (DNA TOPOISOMERASES, TYPE II), with antineoplastic and antitumor activities.

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

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

EGFR-IN-5 is a selective inhibitor of EGFR. The IC50s for EGFR, EGFR(L858R), EGFR(L858R/T790M), and EGFR(L858R/T790M/C797S) are 10.4, 1.1, 34, 7.2 nM, respectively.

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.

Osimertinib mesylate (Mereletinib mesylate) is an irreversible and mutant selective EGFR inhibitor (IC50s: 12/1 nM for EGFR(L858R) and EGFR(L858R/T790M)).

AG490 (Tyrphostin B42) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn, Lck, Syk, Btk, and Src.

Alflutinib (ASK120067) is an inhibitor of EGFR, and its targets including EGFR activating mutations and T790M, thus leading to tumor growth inhibition.

RG13022 (Tyrphostin RG13022) is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM).

Almonertinib (HS-10296) is an inhibitor of EGFR activation mutation and tolerant mutation of EGFR T790M, which has only limited activity against wild-type EGFR.

AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.

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

Afatinib (BIBW 2992) is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively).

Tyrphostin 23 (AG18) inhibits EGFR with IC50 of 35 μM.

PP 3 is a Negative control for the Src kinase inhibitor PP 2

ARRY-380 analog (HER2-Inhibitor-1) is a potent and selective HER2 inhibitor.

AV-412 (MP412) is an EGFR inhibitor (EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M and ErbB2 with IC50s of 0.75, 0.79, 0.5, 2.3, 19 nM).

WHI-P154 (Jak3 inhibitor ii) is a potent JAK3 inhibitor.

AG 555 (Tyrphostin B46) is an EGFR tyrosine kinase inhibitor.

Matuzumab is a humanized monoclonal antibody used in cancer treatment. It has a high affinity for EGFR frequently associated with the growth of blood vessels in malignancy facilitating tumor growth and survival.

Tyrphostin AG30 (AG30) (AG30) is a potent protein tyrosine kinases (PTK) inhibitor.

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.

NRC-2694 is an antagonist of the epidermal growth factor receptor (EGFR). It has anti-cancer and anti-proliferative properties.

RG14620 (Tyrphostin RG14620) is an epidermal growth factor receptor (EGFR) inhibitor.

EBE-A22 (PD153035 Analog 63) is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.

ZD-4190 is a compound that inhibits both the vascular endothelial growth factor receptor 2 (VEGFR2) and the epidermal growth factor receptor (EGFR) signaling pathways, utilized in cancer treatment.

Epertinib hydrochloride (S-22611 hydrochloride) shows potent antitumor activity. Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively.

Theliatinib, a potent and highly selective EGFR inhibitor, with anti-tumor activity. Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively.

PD153035 hydrochloride (ZM 252868) is a effective and selective inhibitor of EGFR (Ki: 5.2 pM, IC50: 29 pM); few influence against FGFR, PGDFR, InsR, CSF-1, and Src.

Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective dual inhibitor of EGFR/HER2 with IC50s of 13 and 38 nM, respectively.

(R)-Afatinib ((R)-BIBW 2992), an isomer of Afatinib, is a potent, orally administered, irreversible inhibitor targeting the ErbB family (EGFR and HER2) with IC50 values of 0.5 nM for EGFR wt, 0.4 nM for EGFR L858R, 10 nM for EGFR L858R/T790M, and 14 nM for HER2. It holds potential for research into esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC), and gastric cancer [1].

ErbB-2-binding peptide (HER2-binding peptide), a tumor-targeting peptide, holds potential for cancer research applications [1].

BMS-599626 (AC480) has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.

Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].

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

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Sapitinib (AZD-8931) , a reversible, ATP competitive inhibitor of EGFR(IC50=4 nM), ErbB2(IC50=3 nM) and ErbB3(IC50=4 nM), is more effective over Gefitinib or Lapatinib against NSCLC cell, 100-fold more specific for the ErbB family over MNK1 and Flt.

Avitinib (AC0010), also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity. Upon oral administration, avitinib covalently binds to and inhibits the activity of mutant forms of EGFR, including the drug-resistant T790M EGFR mutant, which prevents signaling mediated by mutant forms of EGFR. This may both induce cell death and inhibit tumor growth in EGFR-mutated tumor cells. EGFR, a receptor tyrosine kinase that is mutated in a variety of Ys, plays a key role in tumor cell proliferation and tumor vascularization. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced when compared to non-selective EGFR inhibitors, which also inhibit wild-type EGFR.