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-13427
    Allitinib tosylate
    		Inhibitor 99.54%
    Allitinib tosylate (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib tosylate also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib tosylate is an anilino-quinazoline compound and has anti-cancer activity
    Allitinib tosylate
  • HY-139617
    Sec61-IN-3
    		Inhibitor 99.22%
    Sec61-IN-3 is a Sec61 inhibitor. Sec61-IN-3 shows a significant inhibitory effect on PD-1 related reporter gene cell models (PD1tsGluc) (IC50 = 42 nM), and also has certain inhibitory activity on Her3 (IC50 = 99 nM), IL2 (IC50 = 144 nM) related reporter pathways, but has a relatively weak inhibitory effect on the TNFα (IC50 = 580 nM) pathway. Sec61-IN-3 can be used for cancer research.
    Sec61-IN-3
  • HY-147183A
    JBJ-09-063 TFA
    		Inhibitor 99.64%
    JBJ-09-063 TFA 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 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer.
    JBJ-09-063 TFA
  • HY-155079
    DZD1516
    		99.62%
    DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models.
    DZD1516
  • HY-118263
    Dacomitinib hydrate
    		Inhibitor 99.54%
    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-136430
    JCN037
    		Inhibitor 99.09%
    JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively.
    JCN037
  • HY-N1073
    Wighteone
    		Inhibitor 98.71%
    Wighteone (6-Isopentenylgenistein; Erythrinin B) is a prenylated isoflavone that acts as a HSP90/EGFRL858R/T790M inhibitor and antifungal agent. Wighteone reduces the expression level of HSP90, blocks EGF-induced phosphorylation of EGFR, and thereby inhibits the downstream ERK and AKT signaling pathways. Wighteone induces cell cycle redistribution, inhibits proliferation and triggers apoptosis in cancer cells. Wighteone can be isolated from Erythrina suberosa, and can also be induced to synthesize in Lotus japonicus under specific conditions. Wighteone can be used to study HER2-positive breast cancer, leukemia, non-small cell lung cancer with EGFRL858R/T790M mutation, and fungal infections.
    Wighteone
  • HY-153901
    PROTAC EGFR degrader 8
    		Inhibitor 98.90%
    PROTAC EGFR degrader 8 (T-184) is a PROTAC EGFR degrader. PROTAC EGFR degrader 8 degrades EGFR in HCC827 cell with a DC50 of 15.56 nM. PROTAC EGFR degrader 8 inhibits H1975, PC-9, HCC827 cell growth with IC50s of 7.72 nM, 121.9 nM, 14.21 nM. PROTAC EGFR degrader 8 can be used for research of cancer, especially NSCLC.
    PROTAC EGFR degrader 8
  • HY-110406
    13(S)-HPODE
    		Activator
    13(S)-HPODE is a linoleic acid metabolite found in several plants and mammals.
    13(S)-HPODE
  • HY-43533
    Tarlox-TKI
    		Inhibitor 98.79%
    Tarlox-TKI, the active metabolite of Tarloxotinib, is an irreversible pan-ErbB TKI (Tarlox-TKI).
    Tarlox-TKI
  • HY-117155
    PKI-166
    		Inhibitor 98.92%
    PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.
    PKI-166
  • HY-149530
    EGFR-IN-86
    		Inhibitor 99.92%
    EGFR-IN-86 (compound 4i) is an EGFR inhibitor (IC50: 1.5 nM) with high activity against glioblastoma. EGFR-IN-86 induces apoptosis and arrests the U87 cell cycle in the G2/M phase.
    EGFR-IN-86
  • HY-107459
    (E/Z)-AG490
    		Inhibitor 99.71%
    (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
    (E/Z)-AG490
  • HY-161537
    EGFR ligand-9
    		Inhibitor 98.80%
    EGFR ligand-9 is an EGFR ligand. EGFR ligand-9 can be used for synthesis of PROTAC EGFR degrader 9 (HY-161536).
    EGFR ligand-9
  • HY-P5314
    OK2
    		Inhibitor 99.13%
    OK2, a specific inhibitor of the CCN2/EGFR interaction, efficiently blocks CCN2/EGFR interaction through binding to the CT domain of CCN2. OK2 can be used for kidney fibrosis and chronic kidney disease research.
    OK2
  • HY-W018800
    4(3H)-Quinazolinone
    		Inhibitor 99.89%
    4(3H) -quinazolinone is a fused nitrogen heterocyclic compound whose derivatives have a wide range of antimicrobial and antitumor activities.
    4(3H)-Quinazolinone
  • HY-101960A
    Tyrphostin A51
    		Inhibitor 99.0%
    Tyrphostin A51 is a potent protein tyrosine kinase (PTK) inhibitor. Tyrphostin A51 inhibits the volume-dependent release of [3H]taurine in a dose-dependent manner. Tyrphostin A51 markedly reduces cellular tyrosyl phosphorylation level. Tyrphostin A51 inhibits both basal and EGF-induced human bone cell proliferation.
    Tyrphostin A51
  • HY-P4082
    ErbB-2-binding peptide
    		99.52%
    ErbB-2-binding peptide (HER2-binding peptide) is a tumor-binding peptide. ErbB-2-binding peptide has the potential for cancer research.
    ErbB-2-binding peptide
  • HY-101820
    Simotinib
    		Inhibitor 99.39%
    Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
    Simotinib
  • HY-146349
    PROTAC EGFR degrader 4
    		Inhibitor 99.70%
    PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy.
    PROTAC EGFR degrader 4
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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