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

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

EGFR

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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-168064
    EGFR-IN-124
    		Inhibitor
    EGFR-IN-124 (compound 10A) is an EGFR inhibitor, with IC50 of 0.54 μM. EGFR-IN-124 can be used in anti-cancer research.
    EGFR-IN-124
  • HY-123891
    NS-062
    		Inhibitor
    NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC50 of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model.
    NS-062
  • HY-163434
    PRMT5/EGFR-IN-1
    		Inhibitor
    PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors.
    PRMT5/EGFR-IN-1
  • HY-175292
    EGFR WT/T790M-IN-3
    		Inhibitor
    EGFR WT/T790M-IN-3 is an irreversible covalent EGFRWT and EGFRT790M inhibitor with IC50s value of 28.1 and 24.6 nM. EGFR WT/T790M-IN-3 hampers tubulin polymerization through IC50 value of 5.1 μM. EGFR WT/T790M-IN-3 shows significant anti-proliferative effects on HCT116 and T47D cells, with IC50 values of 3.12 and 4.12 μM, respectively. EGFR WT/T790M-IN-3 can be used for the study of cancers such as non-small cell lung cancer, colon cancer and breast cancer.
    EGFR WT/T790M-IN-3
  • HY-173520
    EGFR/HDAC-IN-1
    		Inhibitor
    EGFR/HDAC-IN-1 (Compound 22c2) is a potent dual inhibitor of epidermal growth factor receptor (EGFR) and histone deacetylase (HDAC) with IC50 values of 4.81 nM, 119.4 nM and 354.8 nM for EGFR, HDAC1 and HDAC3, respectively. EGFR/HDAC-IN-1 blocks the EGFR signaling pathway and affects the histone acetylation status, thereby inhibiting tumor cell proliferation. EGFR/HDAC-IN-1 is promising for research of non-small cell lung cancer (NSCLC).
    EGFR/HDAC-IN-1
  • HY-149824
    EGFR T790M/L858R-IN-2
    		Inhibitor 99.66%
    EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis.html" class="link-product" target="_blank">Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity.
    EGFR T790M/L858R-IN-2
  • HY-W777297
    Lapatinib-13C215N
    Lapatinib-13C2,15N Ditosylate is the 13C- and 15N-labeled Lapatinib ditosylate (HY-50898A). Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
    Lapatinib-<sup>13</sup>C<sub>2</sub>15</sup>N</sub>
  • HY-173038
    EGFR-IN-151
    		Inhibitor
    EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. EGFR-IN-151 inhibits the proliferation of a variety lung cancer cells (IC50s for NCI-H1781, HCC827, NCI-H3255 and NCI-H1975 is 11.7, 5.19, 7.32 and 1.53 μM, respectively), inhibits the colony formation and migration of H1975, arrests the cell cycle at G1 phase, and induces apoptosis in H1975.
    EGFR-IN-151
  • HY-161866
    EGFR-IN-118
    		Inhibitor
    EGFR-IN-118 (Compound 4a) is an inhibitor for the tyrosine kinase EGFR. EGFR-IN-118 demonstrates anti-cancer property, inhibiting the proliferation of MCF-7 and PC3 with IC50 of 2.53 and 3.25 µg/ml. EGFR-IN-118 exhibits antioxidant efficacy, inhibiting the DPPH free radicals with IC50 of 10.04 µg/ml.
    EGFR-IN-118
  • HY-100636
    Gefitinib N-oxide
    		Inhibitor
    Gefitinib N-oxide is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
    Gefitinib N-oxide
  • HY-164392
    TAS-121
    		Inhibitor
    TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models.
    TAS-121
  • HY-10261S1
    Afatinib-d4
    		Inhibitor
    Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
    Afatinib-d<sub>4</sub>
  • HY-144052
    EGFR-IN-35
    		Inhibitor
    EGFR-IN-35 is a potent inhibitor of EGFR. EGFR-IN-35 is an anti-tumor agent with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. 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-35 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 11).
    EGFR-IN-35
  • HY-142678
    EGFR-IN-21
    		Inhibitor
    EGFR-IN-21 is a potent EGFR inhibtior with an IC50 of 0.38 nM. EGFR-IN-21 has antitumor activity.
    EGFR-IN-21
  • HY-172877
    EGFR/BRAFV600E-IN-5
    		Inhibitor
    EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC50 of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC50 of 3.16 μM and 2.50 μM against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway.
    EGFR/BRAFV600E-IN-5
  • HY-142681
    EGFR-IN-28
    		Inhibitor
    EGFR-IN-28 is a potent EGFR inhibitor. EGFR-IN-28 has antitumor activity.
    EGFR-IN-28
  • HY-161632
    PROTAC EGFR degrader 10
    		Degrader
    PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a Ki of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <150 nM.
    PROTAC EGFR degrader 10
  • HY-172534
    BPN-01
    		Substrate
    BPN-01 is a fluorescent probe targeting translocator protein (TSPO) and human epidermal growth factor receptor 2 (HER2) with binding affinities of -10.7 kcal/mol for TSPO and -11.3 kcal/mol for HER2. BPN-01 is promising for research of solid tumor imaging during fluorescence image-guided surgery (FIGS) (Ex/Em = 475/510 nm).
    BPN-01
  • HY-P991505
    Anti-HER3 Antibody (Ab562)
    		Antagonist
    Anti-HER3 Antibody (Ab562) is an anti-HER3 monoclonal antibody. Anti-HER3 Antibody (Ab562) can be used to synthesize the antibody-drug conjugate (ADC) AMT-562 (HY-171747).
    Anti-HER3 Antibody (Ab562)
  • HY-151573
    EGFR/CDK2-IN-1
    		Inhibitor
    EGFR/CDK2-IN-1 (Compound 3b) is an EGFR/CDK2 inhibitor. EGFR/CDK2-IN-1 shows good cytotoxicity against MCF7 and HepG2 cells. EGFR/CDK2-IN-1 can be used in cancer research.
    EGFR/CDK2-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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