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-142283
    Dosimertinib-d3
    Inhibitor
    Dosimertinib-d3-d3 is a potent and orally active EGFR inhibitor. Dosimertinib-d3-d3 decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d3-d3 shows antiproliferative and anti-tumor activity. Dosimertinib-d3-d3 has the potential for the research of non-small-cell lung cancer (NSCLC).
    Dosimertinib-d<sub>3</sub>
  • HY-18750A
    Zorifertinib hydrochloride
    Inhibitor
    Zorifertinib (AZD3759) hydrochloride is a potent, orally active, central nervous system-penetrant, EGFR inhibitor (IC50s: 0.3, 0.2, and 0.2 nM for EGFRwt, EGFRL858R, and EGFRexon 19Del, respectively). Zorifertinib hydrochloride induces cancer cell apoptosis. Zorifertinib hydrochloride has antitumor activity, and can be used for NSCLC, HCC etc. research.
    Zorifertinib hydrochloride
  • HY-135914
    JBJ-02-112-05
    Inhibitor
    JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.
    JBJ-02-112-05
  • HY-135815B
    Mobocertinib mesylate
    Inhibitor
    Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research.
    Mobocertinib mesylate
  • HY-50895G
    Gefitinib (GMP)
    Inhibitor
    Gefitinib (ZD1839) (GMP) is Gefitinib (HY-50895) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Gefitinib is a potent, selective and orally active EGFR tyrosine kinase inhibitor.
    Gefitinib (GMP)
  • HY-50898C
    Lapatinib tosylate
    Inhibitor
    Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
    Lapatinib tosylate
  • HY-132883
    EGFR/CSC-IN-1
    Inhibitor
    EGFR/CSC-IN-1 is a potential EGFR (IC50 10.52 nM) and cancer stem cell (CSC) dual inhibitor for triple-negative breast cancer research.
    EGFR/CSC-IN-1
  • HY-144048
    EGFR-IN-31
    EGFR-IN-31 is a potent inhibitor of EGFR. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-31 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185298A1, compound 2).
    EGFR-IN-31
  • HY-118998
    TX2-121-1
    Inhibitor
    TX2-121-1 is a potent and selective Her3 (ErbB3) degrader that contains a hydrophobic adamantane moiety. TX2-121-1 has an IC50 of 49 nM for Her3. TX2-121-1 inhibits Her3-dependent signaling and heterodimerization of Her3. TX2-121-1 has the ability to inhibit cell proliferation. TX2-121-1 can be used in the study of tumors. (Pink: Her3 inhibitor (HY-164988); Black: Linker; Blue: Adamantane (HY-N2427)).
    TX2-121-1
  • HY-B0793S1
    AZ-5104-d2
    Inhibitor
    AZ-5104-d2 is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively.
    AZ-5104-d<sub>2</sub>
  • HY-128860
    Mutated EGFR-IN-2
    Inhibitor
    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=<1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.
    Mutated EGFR-IN-2
  • HY-139920A
    Oritinib mesylate
    Inhibitor
    Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation.
    Oritinib mesylate
  • HY-131067
    EMI56
    Inhibitor 99.72%
    EMI56, the derivative of EMI1, displays greater potency toward mutant EGFR than EMI1. EMI56 inhibits EGFR triple mutants.
    EMI56
  • HY-163354
    EGFR-IN-103
    Inhibitor
    EGFR-IN-103 (compound 1) is a potent EGFR inhibitor with an IC50 of 6 nM for pEGFR.
    EGFR-IN-103
  • HY-143734
    HER2-IN-6
    HER2-IN-6 is a potent inhibitor of HER2. HER2-IN-6 has the potential for the research of wild and/or mutant EGFR and/or HER2 kinase mediated tumor (extracted from patent WO2021164697A1, compound 11).
    HER2-IN-6
  • HY-10251
    BMS-599626
    Inhibitor 98.56%
    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
    BMS-599626
  • HY-131066
    EMI48
    Inhibitor 99.02%
    EMI48, the derivative of EMI1, displays greater potency toward mutant EGFR than EMI1. EMI48 inhibits EGFR triple mutants.
    EMI48
  • HY-P990962
    Vislarafusp alfa
    HY-P990962 is an EGFR/CD47-targeting IgG1κ type humanized antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Vislarafusp alfa
  • HY-P990972
    Azerutamig
    HY-P990972 is an KLRK1/ERBB2-targeting (H-γ1_L-κ)_scFvkh-H-γ1(h-CH2-CH3) type bispecific antibody.
    Azerutamig
  • HY-137433A
    Befotertinib mesylate
    Inhibitor
    Befotertinib (D-0316) mesylate is an orally active EGFR tyrosine kinase inhibitor. Befotertinib mesylate can inhibit the proliferation of tumor cells. Befotertinib mesylate can be used in the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).
    Befotertinib mesylate
Cat. No. Product Name / Synonyms Species Source
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