EGFR

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.

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.

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.

Disitamab vedotin (RC-48) is a newly developed antibody-active molecule conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2), consisting of hertuzumab coupled to monomethyl auristatin E (MMAE) via a cleavable linker. Disitamab vedotin showed anti-tumor and anti-proliferative activities in gastric cancer cells with different HER-2 expression levels and inhibited the expression of HER-2 protein in gastric cancer cells.

Rilzabrutinib (PRN1008) is a reversible covalent, selective, and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK) with an IC50 of 1.3 nM.

Sunvozertinib (DZD9008) is a potent ErbBs and BTK inhibitor, with inhibitory effects on EGFR, Her2, and mutant epidermal growth factor. Sunvozertinib (DZD9008) showed inhibitory effects on EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, as well as Her2 exon 20 YVMA and EGFR WT A431 with IC50 of 20.4, 20.4, 1.1, 7.5, and 80.4 nM.

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

Pyrotinib dimaleate is a selective EGFR HER2 dual inhibitor with IC50 values ​​of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer.

Alflutinib mesylate (AST2818 mesylate) ,is an irreversible tyrosine kinase inhibitor that selectively inhibits EGFR mutations, especially T790M.

SDZ 281-977 is a derivative of Lavendustin A, an EGF receptor tyrosine kinase inhibitor.

Afatinib (BIBW 2992) is an irreversible inhibitor of the 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.

EGFR-IN-76 is a potent EGFR inhibitor.

Cavutilide has antiarrhythmic activity, inhibits hERG K(+) channels, and can be used to study heart failure and persistent atrial fibrillation.

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

BLU-945 is a reversible, potent, highly selective, and orally available epidermal growth factor receptor tyrosine kinase inhibitor (TKIs). BLU-945 inhibits EGFR phosphorylation in EGFR L858R T790M C797S and EGFR ex19del T790M C797S mutant cell lines. BLU-945 can be used in lung cancer research, including non-small cell lung cancer (NSCLC).

Befotertinib (D-0316) is an inhibitor of EGFR tyrosine kinase and can be used for studies about EGFR T790M-positive non-small cell lung cancer.

Labutinib is a selective inhibitor of the c-kit tyrosine kinase [1].

Epidermal Growth Factor binds to epidermal growth factor receptor (EGFR) and stimulates cell growth and proliferation. It is approved for the treatment of diabetic foot ulcers.

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.

(Rac)-JBJ-04-125-02 (JBJ-04-125-02) is effective as a single agent in both in vitro and in vivo models of EGFR-mutant lung cancer.

Pertuzumab (anti-HER2) a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors impairs the ability of HER2 to bind to other members of the HER family.

Desmethyl Erlotinib (CP-473420) is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).

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

Almonertinib (HS-10296) is an inhibitor specifically targeting EGFR activation mutations and the resistant EGFR T790M mutation, exhibiting limited activity against wild-type EGFR.

PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.

DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM for EGFRWT and 48 nM for EGFRL858R T790M, capable of occupying the ATP-binding site and demonstrating significant antitumor efficacy.

Amivantamab (JNJ-61186372) is a humanized antibody that recognizes epidermal growth factor receptor (EGFR) and MET proto-oncogene (MET), with anticancer and anti-tumor activities, preventing ligand binding to EGFR and MET and receptor dimerization that inhibits downstream signal transduction. Amivantamab can induce Fc-dependent endocytosis of macrophages and antibody-dependent cytotoxicity of natural killer cells, and can be used to study metastatic non-small cell lung cancer.

EGFR-IN-7 (TQB3804) is a selective and potent EGFR kinase inhibitor.

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

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.

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.

BGB-102 (JNJ-26483327) is a kinase inhibitor targeting FLT3 and YES1 and an antagonist targeting EGFR and VEGFR3, which may be useful in the study of macular degeneration and diseases associated with genetic disorders and malformations.

Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR HER2.

Lazertinib (GNS-1480) is an effective, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19 T790M, L858R T790M, Del19, L85R and Wild type EGFR respectively.

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.

E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM)

WS3, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.

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.

HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM), effectively suppressing EGFR autophosphorylation (at Y1068), as well as AKT and MAPK phosphorylation.

RTC-5 (TRC-382) is a phenothiazine compound that has been specifically enhanced for its potent anti-cancer properties. It exhibits considerable effectiveness against an EGFR-driven cancer xenograft model. The mechanism behind its efficacy can be attributed to the simultaneous inhibition of PI3K-AKT and RAS-ERK signaling pathways.

Zipalertinib (TAS6417, CLN-081) is a novel, highly potent, orally active covalent EGFR tyrosine kinase inhibitor that uniquely binds to the ATP binding site of the EGFR hinge region with an IC50 value of 1.1-8.0 nM.

Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg mL).

Brigatinib (AP-26113) is a highly potent and selective inhibitor of ALK.

Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R T790M), EGFR (d746-750), EGFR (d746-750 T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer.

BGB-8035 is an orally available, selective and potent BTK inhibitor with antitumor activity that inhibits BTK, TEC and EGFR.BGB-8035 is used in the study of tumors and autoimmune diseases.

Tyrphostin A9 (SF 6847) is an Agricultural acaricide, now superseded. Tyrphostin A9 is firstly designed as an EGFR inhibitor

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.

Icotinib (Conmana) is an orally available quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity.