EGFR

EGFR

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.

EGFR related products

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).
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