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

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-19816A
    Avitinib maleate
    Inhibitor 99.86%
    Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects.
    Avitinib maleate
  • HY-107367A
    Epertinib hydrochloride
    Inhibitor 98.15%
    Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity. Epertinib (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Epertinib hydrochloride
  • HY-147941A
    MS9427 TFA
    Degrader 98.38%
    MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer.
    MS9427 TFA
  • HY-116437
    Selatinib
    Inhibitor 98.56%
    Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects.
    Selatinib
  • 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-162299
    EGFR kinase inhibitor 3
    Inhibitor 99.03%
    EGFR kinase inhibitor 3 (compound 2) is a bivalent ATP-allosteric EGFR kinase inhibitor with IC50s of <10 nM, 1.5 nM, 0.059 nM, 0.064 nM for WT EGFR, EGFR-activating mutations L858R, L858R/T790M and L858R/T790M/C797S, respectively. EGFR kinase inhibitor 3 is a C-linked inhibitor.
    EGFR kinase inhibitor 3
  • 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-B1394
    Khellin
    Inhibitor 99.66%
    Khellin is a furochromone that can be isolated from Ammi visnuga L.. Khellin is an EGFR inhibitor with an IC50 of 0.15 µM. Khelline has anti-proliferative activity in vitro. Khellin has antispasmodic and coronary vasodilator effects.
    Khellin
  • HY-138916
    PF-06672131
    Inhibitor 99.47%
    PF-06672131 is an alkynylated afatinib derivative and a small molecule probe that is reactive to cysteine. PF-06672131 is an inhibitor of epidermal growth factor receptor (EGFR) kinase that targets the ATP pockets of EGFR. PF-06672131 can be used for activity-based protein profiling studies.
    PF-06672131
  • HY-101041
    (E)-AG 556
    Inhibitor 99.91%
    (E)-AG 556 is a highly selective EGFR inhibitor and also blocks LPS-induced TNF-α production.
    (E)-AG 556
  • HY-19803
    Naquotinib mesylate
    Inhibitor 98.05%
    Naquotinib mesylate (ASP8273 mesylate) 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 mesylate
  • 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-15772S
    Osimertinib-d6
    Inhibitor 99.70%
    Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
    Osimertinib-d<sub>6</sub>
  • HY-18603
    FIIN-3
    Inhibitor 99.01%
    FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
    FIIN-3
  • HY-147942
    MS9449
    98.95%
    MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer.
    MS9449
  • HY-128576
    DS21360717
    99.80%
    DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC50 of 0.49 nM. Anti-cancer activity.
    DS21360717
  • 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-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
    98.31%
    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-P990071
    Fepixnebart
    Inhibitor
    Fepixnebart (LY3016859) is a humanized monoclonal hIgG4 antibody, which binds and neutralizes only TGFα and epiregulin with high affinity. Fepixnebart can be used for the study of diabetic nephropathy and broad-spectrum chronic pain, including diabetic peripheral neuropathic pain (DPNP), signs and symptoms of osteoarthritis (OA), and chronic low back pain (CLBP).
    Fepixnebart
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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