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-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-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-107364
    MTX-211
    Inhibitor 99.81%
    MTX-211 (Mol 211) is a dual inhibitor of EGFR and PI3K with IC50 values of <100 nM. MTX-211 can be used for the research of cancer and other diseases.
    MTX-211
  • 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-P990049
    Becotatug
    Inhibitor 98.44%
    Becotatug (JMT-101) is an IgG1 antibody targeting EGFR that can also be conjugated to Afatinib (HY-10261) and Osimertinib (HY-15772) as a synthetic ADC.
    Becotatug
  • HY-130616
    EGFR-IN-11
    Inhibitor 99.30%
    EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.
    EGFR-IN-11
  • HY-120590
    Ruserontinib
    Inhibitor 99.82%
    Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC50 value of 55 nM for human FLT3, and has antitumor activity.
    Ruserontinib
  • HY-P99437
    Anbenitamab
    Inhibitor 99.22%
    Anbenitamab (KN-026) is a bispecific antibody simultaneously targeting the extracellular domains II and IV of the human HER2. Anbenitamab blocks both ligand-dependent and ligand-independent HER2 signaling pathway. The IgG1 Fc fragment of Anbenitamab binds FcRγIIIa mediates potent antibody dependent cell-mediated cytotoxicity (ADCC) and inhibits tumor cell proliferation. Anbenitamab has the potential for HER2-positive metastatic breast cancer (MBC) research.
    Anbenitamab
  • HY-P99866
    Duligotuzumab
    Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody that specifically targets Her3 (ErbB3).
    Duligotuzumab
  • 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-150611
    EGFR-IN-70
    Inhibitor 99.16%
    EGFR-IN-70 (compound 18j) is a potent EGFR inhibitor with IC50 values of 23.6 and 307.5 nM for EGFRLR/TM/CS and EGFRWT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research.
    EGFR-IN-70
  • HY-103442
    CGP52411
    Inhibitor 99.82%
    CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
    CGP52411
  • HY-15375
    Allitinib
    Inhibitor 99.36%
    Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity.
    Allitinib
  • 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-18603
    FIIN-3
    Inhibitor 99.66%
    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-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-139920
    Oritinib
    Inhibitor 99.59%
    Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFRWT, EGFRL858R, EGFRL861Q, EGFRL858R/T790M, EGFRd746-750 and EGFRd746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.
    Oritinib
  • 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-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-43533
    Tarlox-TKI
    Inhibitor 98.84%
    Tarlox-TKI, the active metabolite of Tarloxotinib, is an irreversible pan-ErbB TKI (Tarlox-TKI).
    Tarlox-TKI
Cat. No. Product Name / Synonyms Species Source
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