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-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-135805
    JBJ-04-125-02
    		Inhibitor
    JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
    JBJ-04-125-02
  • 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
    DBPR112
    		Inhibitor 98.37%
    DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy.
    DBPR112
  • HY-115716
    EGFR-IN-17
    		Inhibitor 98.42%
    EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor ( IC50 0.0002 μM) to overcome C797S-mediated resistance.
    EGFR-IN-17
  • HY-P99605
    Cinrebafusp alfa
    		Inhibitor 98.53%
    Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research.
    Cinrebafusp alfa
  • HY-153110
    Larotinib
    		Inhibitor 99.50%
    Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM.
    Larotinib
  • HY-111415
    EGFR-IN-5
    		Inhibitor
    EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively.
    EGFR-IN-5
  • 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[1]. 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-161536
    PROTAC EGFR degrader 9
    		Inhibitor
    PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFRL858R/T790M/C797S. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537)).
    PROTAC EGFR degrader 9
  • HY-126319
    SU5204
    		Inhibitor 99.46%
    SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for VEGFR2/KDR/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-149636
    Multi-target kinase inhibitor 2
    		Inhibitor 99.82%
    Multi-target kinase inhibitor 2 (compound 5K) is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2/KDR/Flk-1, and CDK2 enzymes, with IC50 values ranging from 40 to 204 nM. 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-155005
    EGFR mutant-IN-2
    		Inhibitor
    EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFRL858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFRdel19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity.
    EGFR mutant-IN-2
  • HY-101007A
    (+)-Tyrphostin B44
    		Inhibitor
    (+)-Tyrphostin B44 (Tyrphostin AG 835) (Compound B50) is an EGRF inhibitor with antitumor activities.
    (+)-Tyrphostin B44
  • HY-161126
    EGFR-IN-98
    		Inhibitor
    EGFR-IN-98 (Compound 4c) is a EGFR inhibitor. The IC50 values of L858R/T790M/C797S and Del19/T790M/C797S are 0.277 μM and 0.089 μM, respectively. EGFR-IN 98 can be used in the study of tumors.
    EGFR-IN-98
  • HY-143337
    EGFR-IN-47
    		Inhibitor
    EGFR-IN-47 is a potent and orally active EGFRL858R/T790M/C797S inhibitor with an IC50 of 0.01 μM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC.
    EGFR-IN-47
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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