The receptor tyrosine kinase family of the epidermal growth factor, which also includes HER2/neu (ErbB2), ErbB3 (HER3), and ErbB4 (HER4), includes the epidermal growth factor receptor (EGFR; ErbB1). The extracellular ligand-binding ectodomain, the single chain transmembrane domain, and the intracellular tyrosine kinase domain make up the EGFR, which is located at the cell surface. Epidermal growth factor (EGF), transforming growth factor (TGF-), amphiregulin, heparin-binding EGF, and betacellulin are just a few of the ligands that bind to and activate the EGFR.
The tyrosine kinase domain is activated by the receptors' formation of homo- or heterodimeric complexes after ligand binding. The Ras-Raf-MAP kinase, PI-3K/Akt, PKC, and Stat/Jak signaling pathways are all activated as a result of the dimerization and autophosphorylation of EGFR. The EGFR is activated to control cellular survival, differentiation, and proliferation. The EGFR has been derided as a proto-oncogene primarily because of its function in encouraging cell proliferation and preventing apoptosis.
Structure | Cat No. | Product Name | CAS No. | Product Description |
---|---|---|---|---|
V69395 | Duligotuzumab (MEHD-7945A; RG 7597) | 1314238-96-4 | Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody (mAb) that specifically targets Her3 (ErbB3). | |
V69348 | DZD1516 | 2387570-00-3 | DZD1516 is a potent and specific HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. | |
V2600 | EAI045 | 1942114-09-1 | EAI045 (EAI-045) is a 4th generation selective & allosteric EGFR inhibitor overcoming T790M and C797S resistance. | |
V20419 | EGFR inhibitor | 879127-07-8 | EGFR inhibitor is a novel and potent EGFR inhibitor which directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics. | |
V79256 | EGFR kinase inhibitor 2 | EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S mutants. | ||
V79257 | EGFR mutant-IN-1 | EGFR mutant-IN-1 is a 5-methylpyrimidinone analogue that is a potent and specific inhibitor of EGFRL858R/T790M/C797S mutations with IC50 of 27.5 nM and a significantly lower inhibitory effect on EGFRWT (IC50 > 1.0 μM). | ||
V69386 | EGFR mutant-IN-2 | 2770009-06-6 | EGFR mutant-IN-2 (Compound D51) is an EGFR mutation inhibitor. | |
V69349 | EGFR Protein Tyrosine Kinase Substrate | 945830-38-6 | EGFR PTK (protein tyrosine kinase) Substrate is a substrate of EGFR tyrosine kinase. | |
V77049 | EGFR T790M/L858R-IN-2 | EGFRT790M/L858R-IN-2 is a potent and specific EGFRT790M/L858R inhibitor (antagonist) with IC50s of 3.5 and 1290 nM for EGFRT790M/L858R and EGFR WT respectively. | ||
V69404 | EGFR-IN-1 TFA | 2753348-63-7 | EGFR-IN-1 TFA is an orally bioactive, irreversible, mutant-selective L858R/T790M EGFR inhibitor. | |
V69414 | EGFR-IN-15 | 2573869-16-4 | EGFR-IN-15 (compound I-005) is an EGFR inhibitor (antagonist) with IC50 of 4 nM. | |
V69427 | EGFR-IN-16 | 133550-22-8 | EGFR-IN-16 (compound 3) is a potent EGFR inhibitor (antagonist) with pIC50s of 4.85 and 4.74 for EGFR and HER-2, respectively. | |
V69417 | EGFR-IN-17 | 2817679-31-3 | EGFR-IN-17 is a potent and specific epidermal growth factor receptor (EGFR) inhibitor (IC50 0.0002 μM) designed to overcome C797S-mediated drug resistance. | |
V69367 | EGFR-IN-18 | 2765573-34-8 | EGFR-IN-18 can effectively inhibit the enzymatic activity of L858R/T790M/C797S mutant EGFR (4.9 nM), and the enzymatic activity of wild-type EGFR (47 nM) is also reduced. | |
V69437 | EGFR-IN-22 | 2634646-14-1 | EGFR-IN-22 is a potent EGFR inhibitor (antagonist) with IC50 of 4.91 nM and 0.54 nM against wild-type EGFR and EGFRL858R/T790M/C797S, respectively (CN112538072A, compound 243). | |
V69371 | EGFR-IN-24 | 2757548-54-0 | EGFR-IN-24 is a potent EGFR inhibitor that can suppress EGFR (del19/T790M/C797S) and EGFR (L858R/T790M/C797S) respectively. | |
V69428 | EGFR-IN-45 | 2765560-03-8 | EGFR-IN-45 is a potent pan-inhibitor of epidermal growth factor receptor (EGFR) with IC50s of 0.4 µM and 1.6 µM for EGFR and CDK2, respectively. | |
V69389 | EGFR-IN-48 | 2882851-77-4 | EGFR-IN-48 is a potent and orally bioactive EGFR inhibitor (antagonist) with IC50s of 0.193 nM, 0.251 nM, and 10.4 nM for EGFRd19/TM/CS, EGFRLR/TM/CS, and EGFRWT respectively. | |
V31523 | EGFR-IN-5 | 2225887-26-1 | EGFR-IN-5 is a novel and potent EGFR-TKI with potential anticancer effects. | |
V69430 | EGFR-IN-61 | 2890261-81-9 | EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor (antagonist) with IC50s of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S) and 743 nM (WT). |