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-19617
    EGFR-IN-1
    		Inhibitor
    EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
    EGFR-IN-1
  • HY-147941
    MS9427
    		Degrader
    MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer.
    MS9427
  • HY-147183
    JBJ-09-063
    		Inhibitor
    JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer.
    JBJ-09-063
  • HY-P99628
    Futuximab
    		Inhibitor 98.09%
    Futuximab is a chimeric monoclonal antibody targeting non-overlapping epitopes on EGFR. Futuximab has antineoplastic activity.
    Futuximab
  • HY-130608
    Mutated EGFR-IN-3
    		Inhibitor
    Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.
    Mutated EGFR-IN-3
  • HY-138627
    AST5902
    		Inhibitor
    AST5902 is the active metabolite of Firmonertinib (HY-112870) (EGFR inhibitor). AST5902 has antineoplastic activity.
    AST5902
  • HY-P99888
    Pimurutamab
    		99.42%
    Pimurutamab is a humanized IgG1-κ antibody targeting EGFR. Mainly expressed by CHO-K1 cells.
    Pimurutamab
  • HY-147219
    SIAIS164018
    		Inhibitor
    SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857).
    SIAIS164018
  • HY-128778
    Gozanertinib
    		Inhibitor 98.37%
    Gozanertinib is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy.
    Gozanertinib
  • HY-132842A
    (S)-Sunvozertinib
    		Inhibitor 99.14%
    (S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.
    (S)-Sunvozertinib
  • HY-156741
    EGFR-IN-87
    		Inhibitor
    EGFR-IN-87 (Compound Example 2) is a EGFR tyrosine kinase inhibitor. EGFR-IN-87 has IC50 value of 3.1 nM, 1.3 nM and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790 and EGFR_WT in A431 cells, respectively. EGFR-IN-87 can be used for cancer diseases research.
    EGFR-IN-87
  • HY-50896S
    Erlotinib-d6
    		Inhibitor
    Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Erlotinib-d<sub>6</sub>
  • HY-156741A
    EGFR-IN-87 hydrochloride
    		Inhibitor ≥98.0%
    EGFR-IN-87 (Compound Example 2) hydrochloride is a EGFR tyrosine kinase inhibitor. EGFR-IN-87 hydrochloride has IC50 value of 3.1 nM, 1.3 nM and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790 and EGFR_WT in A431 cells, respectively. EGFR-IN-87 hydrochloride can be used for cancer diseases research.
    EGFR-IN-87 hydrochloride
  • HY-126319
    SU5204
    		Inhibitor 99.46%
    SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.
    SU5204
  • HY-162254
    EGFR/ACK1-IN-1
    		Inhibitor
    EGFR T790M/L858R/ACK1-IN-1 is a dual inhibitor of EGFR T790M/L858R and ACK1. IC50 values are 23 and 263 nM, respectively. EGFR T790M/L858R/ACK1-IN-1 can inhibit cell proliferation and has antitumor activity.
    EGFR/ACK1-IN-1
  • HY-110406
    13(S)-HPODE
    		Activator
    13(S)-HPODE is a linoleic acid metabolite found in several plants and mammals.
    13(S)-HPODE
  • HY-157579
    MS154N
    		99.30%
    MS154N (compound 28) is the negative control of MS39 (HY-157581). MS154N is composed of PROTAC target protein ligand EGFR ligand-11 (HY-168305) (red part), E3 ligase ligand 4-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione (HY-W441376) (blue part) and PROTAC Linker 8-Iodooctan-1-amine (HY-168306) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Me-Thalidomide-O-C8-NH2 (HY-168307).
    MS154N
  • HY-149636
    Multi-target kinase inhibitor 2
    		Inhibitor 99.82%
    Multi-target kinase inhibitor 2 is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values of 79 nM, 40 nM,136 nM, and 204 nM, respectively. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells.
    Multi-target kinase inhibitor 2
  • HY-P1855
    HER2/neu (654-662) GP2
    		98.26%
    HER2/neu (654-662) GP2 is a nine amino acid peptide derived from the human epidermal growth factor receptor 2 (HER2/nue, 654–662), induces HLA-A2-restricted cytotoxic T lymphocytes (CTL) reactive to various epithelial cancers.
    HER2/neu (654-662) GP2
  • HY-100064
    O-Desmethyl gefitinib
    		Inhibitor 99.40%
    O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays.
    O-Desmethyl gefitinib
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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