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-12026
    WZ4002
    		Inhibitor 99.76%
    WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFRL858R, EGFRL858R/T790M, EGFRE746_A750 and EGFRE746_A750/T790M, respectively.
    WZ4002
  • HY-15844
    AG-825
    		Inhibitor 98.02%
    AG-825 (Tyrphostin AG-825) is a selective and ATP-competitive ErbB2 inhibitor which suppresses tyrosine phosphorylation, with an IC50 of 0.35 μM. AG-825 displays anti-cancer activity. AG825 significantly accelerates apoptosis of human neutrophils. AG-825 is a potential agent for overcoming Mn-induced neurotoxicity or AD development.
    AG-825
  • HY-P99406
    Petosemtamab
    		Degrader
    Petosemtamab (MCLA 158) is an anti- EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC).
    Petosemtamab
  • HY-15196
    TAK-285
    		Inhibitor 99.70%
    TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
    TAK-285
  • HY-12872
    Nazartinib
    		Inhibitor 99.03%
    Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively.
    Nazartinib
  • HY-W016412
    Coenzyme Q0
    		Inhibitor 99.88%
    Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling.
    Coenzyme Q0
  • HY-19816
    Avitinib
    		Inhibitor 99.90%
    Avitinib (Abivertinib) 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 is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib shows anticancer effects.
    Avitinib
  • HY-10045
    AEE788
    		Inhibitor 99.13%
    AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.
    AEE788
  • HY-147183B
    JBJ-09-063 hydrochloride
    		Inhibitor 99.37%
    JBJ-09-063 hydrochloride 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 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer.
    JBJ-09-063 hydrochloride
  • HY-136789
    Tuxobertinib
    		Inhibitor 99.90%
    Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.
    Tuxobertinib
  • HY-19816A
    Avitinib maleate
    		Inhibitor ≥98.0%
    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-12972
    Mavelertinib
    		Inhibitor 99.34%
    Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).
    Mavelertinib
  • HY-P9969
    Matuzumab
    Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth.
    Matuzumab
  • HY-109189
    Rezivertinib
    		Inhibitor 99.43%
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
    Rezivertinib
  • HY-P99041A
    Panitumumab (anti-EGFR)
    		Inhibitor 98.00%
    Panitumumab (anti-EGFR) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab (anti-EGFR) inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab (anti-EGFR) can be used in the research of cancers, such as colon cancer.
    Panitumumab (anti-EGFR)
  • HY-108052
    Delphinidin 3-glucoside chloride
    		Inhibitor 99.89%
    Delphinidin 3-glucoside chloride (Delphinidin 3-O-glucoside chloride) is an active anthocyanin found in Hibiscus sabdariffa extract. Delphinidin 3-glucoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL). Delphinidin 3-glucoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC50 of 9.7 μM. Delphinidin-3-O-glucoside chloride inhibits EGFR with an IC50 of 2.37 µM. Delphinidin 3-glucoside chloride exhibits antitumor effects through pAKT/IRF1/HOTAIR pathway. Delphinidin 3-glucoside chloride exhibits efficacy against oxidative stress, inhibits platelet activation and endothelial dysfunction.
    Delphinidin 3-glucoside chloride
  • HY-N2450
    Sulforaphene
    		Inhibitor 99.80%
    Sulforaphene, isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10-4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1/2, NF‐κB and other signals.
    Sulforaphene
  • HY-P99304
    Lumretuzumab
    		Inhibitor ≥99.0%
    Lumretuzumab (Anti-Human ERBB3 Recombinant Antibody) is a humanized anti-HER3 (ERBB3) monoclonal antibody that can be used for the research of cancer.
    Lumretuzumab
  • HY-10322
    Falnidamol
    		Inhibitor 99.05%
    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-19985
    PF-06459988
    		Inhibitor 98.87%
    PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of EGFR mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer.
    PF-06459988
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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