2. Signaling Pathways
  3. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  4. EGFR

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

EGFR

Related Products

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The EGFR family of receptor tyrosine kinases (RTK) comprises four distinct receptors: the EGFR (also known as ErbB-1/HER1), ErbB-2 (neu, HER2), ErbB-3 (HER3) and ErbB-4 (HER4). All EGFR family members are characterized by a modular structure consisting of an extracellular ligand-binding domain, a single hydrophobic transmembrane region, and the intracellular part harbouring the highly conserved tyrosine kinase domain. The ErbB family of receptor tyrosine kinases (RTKs) couples binding of extracellular growth factor ligands to intracellular signaling pathways regulating diverse biologic responses, including proliferation, differentiation, cell motility, and survival. Ten growth factors and their ErbB specificities are: EGF, amphiregulin (AR), and TGF bind ErbB-1; betacellulin, and epiregulin bind both ErbB-1 and ErbB-4; the neuregulins (also called heregulins and Neu differentiation factors) NRG-1 and NRG-2 bind ErbB-3 and ErbB-4; and NRG-3 and NRG-4 bind ErbB-4. No known ligand binds ErbB-2. The three best characterized signaling pathways induced through ErbBs are Ras-mitogen-activated protein kinase (Ras-MAPK), phosphatidylinositol 3 kinase-protein kinase B (PI3K-PKB/Akt), and phospholipase C-protein kinase C (PLC-PKC) pathways.

EGFR Isoform Specific Products:

EGFR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-144048
    EGFR-IN-31
    EGFR-IN-31 is a potent inhibitor of EGFR. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-31 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185298A1, compound 2).
    EGFR-IN-31
  • HY-118998
    TX2-121-1
    		Inhibitor
    TX2-121-1 is a potent and selective Her3 (ErbB3) degrader that contains a hydrophobic adamantane moiety. TX2-121-1 has an IC50 of 49 nM for Her3. TX2-121-1 inhibits Her3-dependent signaling and heterodimerization of Her3. TX2-121-1 has the ability to inhibit cell proliferation. TX2-121-1 can be used in the study of tumors. (Pink: Her3 inhibitor (HY-164988); Black: Linker; Blue: Adamantane (HY-N2427)).
    TX2-121-1
  • HY-B0793S1
    AZ-5104-d2
    		Inhibitor
    AZ-5104-d2 is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively.
    AZ-5104-d<sub>2</sub>
  • HY-128860
    Mutated EGFR-IN-2
    		Inhibitor
    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=＜1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.
    Mutated EGFR-IN-2
  • HY-139920A
    Oritinib mesylate
    		Inhibitor
    Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation.
    Oritinib mesylate
  • HY-131067
    EMI56
    		Inhibitor 99.72%
    EMI56, the derivative of EMI1, displays greater potency toward mutant EGFR than EMI1. EMI56 inhibits EGFR triple mutants.
    EMI56
  • HY-163354
    EGFR-IN-103
    		Inhibitor
    EGFR-IN-103 (compound 1) is a potent EGFR inhibitor with an IC50 of 6 nM for pEGFR.
    EGFR-IN-103
  • HY-143734
    HER2-IN-6
    HER2-IN-6 is a potent inhibitor of HER2. HER2-IN-6 has the potential for the research of wild and/or mutant EGFR and/or HER2 kinase mediated tumor (extracted from patent WO2021164697A1, compound 11).
    HER2-IN-6
  • HY-10251
    BMS-599626
    		Inhibitor
    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
    BMS-599626
  • HY-131066
    EMI48
    		Inhibitor 99.02%
    EMI48, the derivative of EMI1, displays greater potency toward mutant EGFR than EMI1. EMI48 inhibits EGFR triple mutants.
    EMI48
  • HY-P990962
    Vislarafusp alfa
    HY-P990962 is an EGFR/CD47-targeting IgG1κ type humanized antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Vislarafusp alfa
  • HY-P990972
    Azerutamig
    HY-P990972 is an KLRK1/ERBB2-targeting (H-γ1_L-κ)_scFvkh-H-γ1(h-CH2-CH3) type bispecific antibody.
    Azerutamig
  • HY-137433A
    Befotertinib mesylate
    		Inhibitor
    Befotertinib (D-0316) mesylate is an orally active EGFR tyrosine kinase inhibitor. Befotertinib mesylate can inhibit the proliferation of tumor cells. Befotertinib mesylate can be used in the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).
    Befotertinib mesylate
  • HY-10530A
    Varlitinib tosylate
    		Inhibitor
    Varlitinib (ASLAN001) tosylate is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.
    Varlitinib tosylate
  • HY-138746
    EGFR-IN-15
    		Inhibitor
    EGFR-IN-15 (compound I-005) is a EGFR inhibitor with an IC50 of 4 nM. EGFR-IN-15 can be used for oncological diseases research.
    EGFR-IN-15
  • HY-115951
    EGFR/HER2-IN-2
    		Inhibitor
    EGFR/HER2-IN-2 (Compound ZINC35560729) is a dual inhibitor of EGFR and HER2 with IC50 values of 5.02 µM and 0.83 µM against EGFR and HER2, respectively.
    EGFR/HER2-IN-2
  • HY-125841
    EGFR mutant-IN-1
    		Inhibitor
    EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM).
    EGFR mutant-IN-1
  • HY-P99831
    Coprelotamab
    Coprelotamab (GB-221) is an IgG-κ monoclonal antibody targeting EGFR2. The commonly used expression system for Coprelotamab is CHO DG44 (Chinese Hamster Ovary) cells.
    Coprelotamab
  • HY-147407
    Imbotolimod
    		Inhibitor
    Imbotolimod, immunoglobulin G1-kappa, is a humanized monoclonal antibody with anti-ERBB2 and antineoplastic activity. Imbotolimod is a derivative of telratolimod.
    Imbotolimod
  • HY-147303
    Sacibertinib
    		Inhibitor
    Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity.
    Sacibertinib
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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