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-139300A
    Epitinib succinate
    		Inhibitor 99.01%
    Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer. Epitinib (succinate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Epitinib succinate
  • HY-128778
    Gozanertinib
    		Inhibitor 98.37%
    Gozanertinib is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy.
    Gozanertinib
  • HY-132842A
    (S)-Sunvozertinib
    		Inhibitor 99.05%
    (S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.
    (S)-Sunvozertinib
  • HY-115716
    EGFR-IN-17
    		Inhibitor 98.18%
    EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor ( IC50 0.0002 μM) to overcome C797S-mediated resistance.
    EGFR-IN-17
  • HY-P990978
    Caxmotabart
    HY-P990978 is an ERBB2-targeting IgG1κ type humanized antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Caxmotabart
  • HY-P990909
    Calotatug
    		98%
    HY-P990909 is an ERBB2-targeting IgG1κ type human antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Calotatug
  • HY-141481
    DP-C-4
    		Inhibitor 98.15%
    DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP.
    DP-C-4
  • HY-10261S
    Afatinib-d6
    		Inhibitor 99.0%
    Afatinib-d6 (BIBW 2992-d6) is deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor.
    Afatinib-d<sub>6</sub>
  • HY-156741
    EGFR-IN-87
    		Inhibitor
    EGFR-IN-87 (Compound Example 2) is a EGFR tyrosine kinase inhibitor. EGFR-IN-87 has IC50 value of 3.1 nM, 1.3 nM and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790 and EGFR_WT in A431 cells, respectively. EGFR-IN-87 can be used for cancer diseases research.
    EGFR-IN-87
  • HY-131088
    N3-PEG8-Phe-Lys-PABC-Gefitinib
    		Inhibitor
    N3-PEG8-Phe-Lys-PABC-Gefitinib is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (HY-50895) (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC. N3-PEG8-Phe-Lys-PABC-Gefitinib is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    N3-PEG8-Phe-Lys-PABC-Gefitinib
  • HY-145960
    MC-Val-Cit-PAB-Amide-TLR7 agonist 4
    		Agonist 99.39%
    MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate.
    MC-Val-Cit-PAB-Amide-TLR7 agonist 4
  • HY-P992128
    Rinumafusp alfa
    		Inhibitor
    Rinumafusp alfa is a human monoclonal antibody targeting ERBB3/HER3. The corresponding isotype control is: Human IgG1 kappa, Isotype Control (HY-P99001).
    Rinumafusp alfa
  • HY-126850
    4-Epidoxycycline
    4-Epidoxycycline is a liver metabolite of the antibiotic doxycycline (doxycycline, HY-N0565) and doesn't have antibiotic properties in mice. 4-Epidoxycycline’s ability to regulate HER2 gene expression in vitro and in live mouse models is similar to that of doxycycline, and it shows comparable high efficacy in tumor tissues, achieving over 95% tumor regression rates.
    4-Epidoxycycline
  • HY-131088A
    N3-PEG8-Phe-Lys-PABC-Gefitinib TFA
    		Inhibitor
    N3-PEG8-Phe-Lys-PABC-Gefitinib TFA is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (HY-50895) (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC. N3-PEG8-Phe-Lys-PABC-Gefitinib TFA is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    N3-PEG8-Phe-Lys-PABC-Gefitinib TFA
  • HY-P991507
    SCT200
    		Inhibitor 99.09%
    SCT200 is a fully humanized IgG1 anti-EGFR monoclonal antibody with a Kd of 0.08 nM. SCT200 can kill tumor cells by complement-dependent cytotoxicity (CDC) and antibody-dependent cellular cytotoxicity (ADCC) through the Fc. SCT200 can be used for the study of refractory RAS and BRAF wild-type metastatic colorectal cancer.
    SCT200
  • HY-126319
    SU5204
    		Inhibitor 99.46%
    SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.
    SU5204
  • HY-162254
    EGFR/ACK1-IN-1
    		Inhibitor 98.19%
    EGFR T790M/L858R/ACK1-IN-1 is a dual inhibitor of EGFR T790M/L858R and ACK1. IC50 values are 23 and 263 nM, respectively. EGFR T790M/L858R/ACK1-IN-1 can inhibit cell proliferation and has antitumor activity.
    EGFR/ACK1-IN-1
  • HY-P991780
    Anti-Mouse HER2 (domain I) Antibody (H2Mab-304)
    		Inhibitor
    Anti-Mouse HER2 (domain I) Antibody (H2Mab-304) reacts with domain I of mouse HER2. HER2 is a 185 kDa transmembrane receptor tyrosine kinase that is part of the EGFR family. Recommend Isotype Controls: Rat IgG1 kappa, Isotype Control (HY-P99979).
    Anti-Mouse HER2 (domain I) Antibody (H2Mab-304)
  • HY-149636
    Multi-target kinase inhibitor 2
    		Inhibitor 99.82%
    Multi-target kinase inhibitor 2 is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values of 79 nM, 40 nM,136 nM, and 204 nM, respectively. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells.
    Multi-target kinase inhibitor 2
  • HY-P990695
    Lunaxafusp
    		Inhibitor
    Lunaxafusp is an anti-ERBB2 scFv-heavy-κ monoclonal antibody composed of a single chain variable fragment, an antibody heavy chain, and a kappa antibody light chain.
    Lunaxafusp
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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