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-13501
    Mubritinib
    Inhibitor 99.91%
    Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM.
    Mubritinib
  • HY-132842
    Sunvozertinib
    Inhibitor 99.62%
    Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52).
    Sunvozertinib
  • HY-12461
    WS6
    Activator 99.09%
    WS6 is an IkB kinase and EBP1 inhibitor, with IC50 values of 0.24 nM, 0.21 nM, and 40.48 nM in MV4-11, MOLM13, and K562 cells, respectively. WS6 promotes the proliferation of alpha and beta cells in the pancreas, has antioxidant and anti-inflammatory activities, and can alleviate depression like behavior in rats[1][2][4].
    WS6
  • HY-135815
    Mobocertinib
    Inhibitor 99.60%
    Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research.
    Mobocertinib
  • HY-P99386
    Vesencumab
    Inhibitor 99.34%
    Vesencumab (MNRP-1685A) is IG1 antibody against neuropilin-1 (NRP-1). Vesencumab binds to NRP-1 and prevents the subsequent coupling of NRP-1 to VEGFR-2. Vesencumab has anti-angiogenic and anti-neoplastic activities. Vesencumab can be used in the research of metastatic solid tumors, including ovarian cancer.
    Vesencumab
  • HY-100958
    4-DAMP
    Inhibitor 99.96%
    4-DAMP (4-DAMP methiodide) is a potent and selective antagonist of M3 receptors and also has a high affinity for the closely-related M5 receptors. 4-DAMP combined with 5-Fluorouracil (5-Fu) (HY-90006) could significantly reduce the cell viability and enhance apoptosis in MKN45 and BGC823 gastric cancer cells. 4-DAMP inhibits lipopolysaccharide (LPS)- and tobacco-induced pulmonary inflammation and reduces mucin 5AC (MUC5AC), oligomeric mucus/gel-forming secretion.
    4-DAMP
  • HY-P99854
    Disitamab
    Inhibitor 98.70%
    Disitamab (RC48-0) is a humanized monoclonal antibody targeting HER2. Disitamab can be used in the synthesis of antibody-drug conjugates (ADCs), Disitamab vedotin (HY-P9985).
    Disitamab
  • HY-P99041A
    Panitumumab (anti-EGFR)
    Inhibitor 99.02%
    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-171265
    Becotatug vedotin
    Degrader
    Becotatug vedotin (MRG003) is an Antibody-Drug Conjugate (ADC) that consists of an anti-EGFR humanized IgG1 monoclonal antibody Becotatug (HY-P990049) and MMAE (HY-15162). These two parts are connected through a valine-citrulline (valine-citrulline) linker, where the linker and MMAE constitute the ADC's Drug-Linker conjugate VcMMAE (HY-15575).
    Becotatug vedotin
  • HY-79077
    Osimertinib dimesylate
    Inhibitor 99.96%
    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
    Osimertinib dimesylate
  • HY-32721B
    Neratinib maleate
    Inhibitor 99.74%
    Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively.
    Neratinib maleate
  • HY-164718
    Sevabertinib
    Inhibitor 99.90%
    Sevabertinib (BAY 2927088) is an orally active and reversible dual EGFR-HER2 inhibitor (IC50 <0.5 nM for wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD). Sevabertinib has anticancer activity against lung cancer.
    Sevabertinib
  • HY-32718
    Pelitinib
    Inhibitor 99.13%
    Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
    Pelitinib
  • HY-15730
    Poziotinib
    Inhibitor 99.96%
    Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFRwt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFRT790M and EGFRL858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity.
    Poziotinib
  • HY-15729
    Rociletinib
    Inhibitor 99.67%
    Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
    Rociletinib
  • HY-50898A
    Lapatinib ditosylate
    Inhibitor 99.98%
    Lapatinib ditosylate (GW572016 ditosylate) 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 ditosylate
  • HY-P9969
    Matuzumab
    98.12%
    Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth. Deglycosylation and the possible elimination of ADCC activity can reduce the in vivo anti-tumor activity of Mattuzumab.
    Matuzumab
  • HY-B0793
    AZ-5104
    Inhibitor 99.91%
    AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively.
    AZ-5104
  • HY-156698
    HJM-561
    Degrader 99.26%
    HJM-561 is a selective and effective orally active EGFR PROTAC degrader. HJM-561 is able to overcome the triple EGFR mutations that are resistant to Osimertinib (HY-15772). HJM-561 exhibits potent degradation of EGFR Del19/T790M/C797S (DC50: 9.2 nM) and L858R/T790M/C797S (DC50: 5.8 nM), and has anti-tumor activity (pink: EGFR ligand (HY-12857); blue: CRBN ligand (HY-A0003); black: linker).
    HJM-561
  • HY-18957
    Lifirafenib
    Inhibitor 98.01%
    Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
    Lifirafenib
Cat. No. Product Name / Synonyms Species Source
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