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-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-RS04209
    EGFR Human Pre-designed siRNA Set A
    Inhibitor

    EGFR Human Pre-designed siRNA Set A contains three designed siRNAs for EGFR gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    EGFR Human Pre-designed siRNA Set A
  • 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-50896S
    Erlotinib-d6
    Inhibitor
    Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Erlotinib-d<sub>6</sub>
  • HY-156741A
    EGFR-IN-87 hydrochloride
    Inhibitor 98.0%
    EGFR-IN-87 (Compound Example 2) hydrochloride is a EGFR tyrosine kinase inhibitor. EGFR-IN-87 hydrochloride 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 hydrochloride can be used for cancer diseases research.
    EGFR-IN-87 hydrochloride
  • HY-P991238
    MEDI4276 Antibody
    Inhibitor
    MEDI4276 Antibody is an HER2-targeted antibody, which can be used for the synthesis of the ADC molecule MEDI4276. MEDI4276 Antibody can be used in the study of cancer.
    MEDI4276 Antibody
  • 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-P991662
    AMG-595 Antibody
    AMG-595 Antibody is a EGFRvIII targeting antibody. AMG-595 Antibody can be used for synthesis of ADC AMG-595.
    AMG-595 Antibody
  • 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-P991237
    Nezutatug
    Inhibitor 99.9%
    Nezutatug (HMBD-001) is a humanized IgG1 monoclonal antibody inhibitor targeting HER3. Nezutatug inhibits the dimerization of HER3 and inhibits the growth, proliferation and other activities of tumor cells. Nezutatug is promising for research of cancers, such as pancreatic cancer and non-small cell lung cancer.
    Nezutatug
  • HY-100064
    O-Desmethyl gefitinib
    Inhibitor 99.40%
    O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays.
    O-Desmethyl gefitinib
  • HY-155005
    EGFR mutant-IN-2
    Inhibitor
    EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFRL858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFRdel19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity.
    EGFR mutant-IN-2
  • HY-101007A
    (+)-Tyrphostin B44
    Inhibitor
    (+)-Tyrphostin B44 (Tyrphostin AG 835) (Compound B50) is an EGRF inhibitor with antitumor activities.
    (+)-Tyrphostin B44
  • HY-P990697
    Anvatabart
    Inhibitor
    Anvatabart is an anti-ERBB2 human IgG1 κ monoclonal antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
    Anvatabart
  • HY-12872B
    Nazartinib S-enantiomer
    98.66%
    Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor.
    Nazartinib S-enantiomer
  • HY-161618
    MJ04
    Inhibitor 98.08%
    MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg).
    MJ04
  • HY-N6651
    Isocryptotanshinone
    Inhibitor ≥98.0%
    Isocryptotanshinone is a dual STAT3 and PTP1B (IC50 = 56.1 μM) inhibitor. Isocryptotanshinone inhibits STAT3 by binding to the STAT3 SH2 domain to block phosphorylation and nuclear translocation[1][2]. Isocryptotanshinone exerts its anti-proliferative effect via the induction of cell cycle arrest, apoptosis, and pro-death autophagy, through the regulation of STAT3, AKT/mTOR and MAPK signaling pathways[1][3][4]. Isocryptotanshinone suppresses the xenograft gastric cancer (GC) tumor growth in BALB/c nude mice. Isocryptotanshinone can be used for cancer research, such as lung cancer, breast cancer and GC[1][3][4].
    Isocryptotanshinone
  • HY-50895S1
    Gefitinib-d6
    Inhibitor 98.0%
    Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
    Gefitinib-d<sub>6</sub>
  • HY-P11078A
    LARLLT TFA
    99.89%
    LARLLT TFA is an EGFR-binding peptide. LARLLT has the potential for research of EGFR overexpressing cancers, such as lung, ovarian and colorectal cancer.
    LARLLT TFA
  • HY-155358
    Os30
    Inhibitor 98.34%
    Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation.
    Os30
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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