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-137191
    CH7233163
    		Inhibitor 99.61%
    CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities.
    CH7233163
  • HY-118263
    Dacomitinib hydrate
    		Inhibitor 99.03%
    Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC).
    Dacomitinib hydrate
  • HY-142283AS
    Dosimertinib-d5 mesylate
    		Inhibitor 99.44%
    Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
    Dosimertinib-d<sub>5</sub> mesylate
  • HY-43533
    Tarlox-TKI
    		Inhibitor 98.84%
    Tarlox-TKI, the active metabolite of Tarloxotinib, is an irreversible pan-ErbB TKI (Tarlox-TKI).
    Tarlox-TKI
  • HY-155537
    YK-029A
    		Inhibitor 99.50%
    YK-029A is an orally active inhibitor of mutant EGFR，targeting to both the T790M mutations (EGFRT790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity，and results tumor regression in EGFRex20ins-driven PDX models.
    YK-029A
  • HY-N1166
    Tephrosin
    		98.02%
    Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors.
    Tephrosin
  • HY-10261B
    (E/Z)-Afatinib
    		Inhibitor 99.98%
    (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.
    (E/Z)-Afatinib
  • HY-78869
    Mutated EGFR-IN-1
    		Inhibitor 99.84%
    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
    Mutated EGFR-IN-1
  • HY-141640
    MS154
    		Inhibitor 98.80%
    MS154 is a first-in-class E3 ligase cereblon-recruiting EGFR degrader with Kds of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutants. MS154 potently inhibits cell proliferation in lung cancer cells.
    MS154
  • HY-12013
    PD153035 Hydrochloride
    		Inhibitor 99.48%
    PD153035 Hydrochloride (SU-5271 Hydrochloride) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.
    PD153035 Hydrochloride
  • HY-15769
    WHI-P180
    		Inhibitor 99.62%
    WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, VEGFR2/KDR/Flk-1 and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
    WHI-P180
  • HY-147219A
    SIAIS164018 hydrochloride
    		Inhibitor 99.84%
    SIAIS164018 hydrochloride 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 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857).
    SIAIS164018 hydrochloride
  • HY-32721B
    Neratinib maleate
    		Inhibitor 99.83%
    Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively.
    Neratinib maleate
  • HY-103443
    HKI-357
    		Inhibitor 99.65%
    HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
    HKI-357
  • HY-103440
    EGFR/ErbB-2/ErbB-4 inhibitor-3
    		Inhibitor 98.19%
    EGFR/ErbB-2/ErbB-4 inhibitor-3 (compound 29) is a potent tyrosine kinase inhibitor with IC50s of 0.3, 1.1, 0.5, 2.5, 24 nM for erbB1, erbB2, erbB4, EGF, HER, respectively. EGFR/ErbB-2/ErbB-4 inhibitor-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    EGFR/ErbB-2/ErbB-4 inhibitor-3
  • HY-15801
    HG-14-10-04
    		Inhibitor 99.09%
    HG-14-10-04 is a potent ALK and mutant EGFR inhibitor with IC50s of 20 nM, 15.6 nM, 22.6 nM and 124.5 nM for ALK, EGFRLR/TM, EGFR19del/TM/CS and EGFRLR/TM/CS, respectively. HG-14-10-04 can be used to research anticancer.
    HG-14-10-04
  • HY-19729
    Naquotinib
    		Inhibitor 98.71%
    Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
    Naquotinib
  • HY-19815
    Olafertinib
    		Inhibitor 99.51%
    Olafertinib is a third-generation EGFR TKI, with GI50 values of 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19) and 689 nM (EGFR WT), respectively. Olafertinib has the potential for NSCLC research.
    Olafertinib
  • HY-12029
    WZ8040
    		Inhibitor 99.22%
    WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal.
    WZ8040
  • HY-153110A
    Larotinib mesylate hydrate
    		Inhibitor 98.66%
    Larotinib mesylate hydrate 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 mesylate hydrate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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