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-P99437
    Anbenitamab
    		Inhibitor 99.22%
    Anbenitamab (KN-026) is a bispecific antibody simultaneously targeting extracellular domains II and IV of human HER2. Anbenitamab blocks both ligand-dependent and ligand-independent HER2 signaling pathways. Anbenitamab mediates antibody-dependent cellular cytotoxicity (ADCC) via FcγIIIa binding. Ambrinitumab can be used in research for lung cancer, HER2-positive metastatic breast cancer (MBC), gastric cancer, and gastroesophageal junction cancer.
    Anbenitamab
  • HY-15844
    AG-825
    		Inhibitor 98.02%
    AG-825 is a selective, ATP-competitive, tyrosine phosphorylation ErbB2 inhibitor with an IC50 of 0.35 μM. AG825 significantly accelerates Apoptosis of human neutrophils. AG-825 increases β1AR density. AAG-825 has anticancer and anti-inflammatory activities. AAG-825 can be used in cardiovascular disease research.
    AG-825
  • HY-N0211
    Cyasterone
    		Inhibitor 99.58%
    Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors.
    Cyasterone
  • HY-10322
    Falnidamol
    		Inhibitor 99.41%
    Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
    Falnidamol
  • HY-141640
    MS154
    		Inhibitor 99.42%
    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 induces the degradation of mutant but not wild-type EGFR in an E3 ligase-dependent manner in cancer cell lines. MS154 potently inhibits cell proliferation in lung cancer cells (Blue: E3 Ligase ligand (HY-103596); Black: linker (HY-W096167); Pink: EGFR ligand (HY-168305)).
    MS154
  • 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-111138
    CZC-8004
    		Inhibitor 99.81%
    CZC-8004 (CZC-00008004) is a pan-kinase inhibitor. CZC-8004 has IC50 values of 650 and 437 nM for EGFR WT and VEGFR2 V916M, respectively. CZC-8004 can be used in the study of cancer.
    CZC-8004
  • HY-N2184
    Furanodienone
    		99.90%
    Furanodienone is one of the major bioactive constituents derived from Rhizoma Curcumae. Furanodienone induced apoptosis.
    Furanodienone
  • HY-10325
    CL-387785
    		Inhibitor 98.05%
    CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370 pM.
    CL-387785
  • HY-P1845A
    PACAP-38 (31-38), human, mouse, rat TFA
    		Inducer 98.33%
    PACAP-38 (31-38), human, mouse, rat TFA is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat TFA elevates cytosolic Ca2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat TFA demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat TFA can be used for neurotrophic and neuroprotective research.
    PACAP-38 (31-38), human, mouse, rat TFA
  • HY-W087187
    DOTAGA-anhydride
    		99.80%
    DOTAGA-anhydride is a DOTA-based metal chelator that can bind to radionuclides and is used to prepare radionuclide drug conjugates (RDCs). DOTAGA-anhydride can be used to label monoclonal antibodies (mAbs) such as trastuzumab (targeting HER2/neu receptor with an affinity of 5.5 nM) under mild conditions (PBS pH 7.4, 25 °C, 30 minutes) after chelation with indium-111. [111In-DOTAGA]-trastuzumab showed a tumor uptake of 65% ID/g in mice bearing breast cancer BT-474 xenografts 72 hours after injection, which is valuable for SPECT/CT imaging and biodistribution studies.
    DOTAGA-anhydride
  • HY-78869
    Mutated EGFR-IN-1
    		Inhibitor 99.90%
    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-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-20878
    Tyrphostin AG 879
    		Inhibitor 99.85%
    Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity.
    Tyrphostin AG 879
  • 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-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-13895
    WHI-P154
    		Inhibitor 98.77%
    WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.
    WHI-P154
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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