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-12010
    BMS-599626 Hydrochloride
    		Inhibitor 99.68%
    BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
    BMS-599626 Hydrochloride
  • HY-130616
    EGFR-IN-11
    		Inhibitor 99.30%
    EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.
    EGFR-IN-11
  • HY-P99684
    Laprituximab
    		Inhibitor 99.71%
    Laprituximab (J2898A) is a humanized IgG1 anti-EGFR antibody that can be used for the synthesis of ADC IMGN289.
    Laprituximab
  • HY-120590
    Ruserontinib
    		Inhibitor 99.82%
    Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC50 value of 55 nM for human FLT3, and has antitumor activity.
    Ruserontinib
  • HY-P990314
    AFM24
    		Inhibitor
    AFM24 is a bispecific antibody with a TandAb structure expressed in CHO, targeting EGFR&Fc-gamma-RIIIA. AFM24 contains a huIgG1-SCFV heavy chain and a λ light chain, with a predicted molecular weight (MW) of 74.5 kDa. The isotype control for AFM24 can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    AFM24
  • HY-115481
    EphB1-IN-1
    		Inhibitor 99.87%
    EphB1-IN-1 (Compound 1) is a potent EphB1 inhibitor with IC50s of 3.0, 15 and 220 nM against EphB1G703C, EphB1T697G and EphB1WT, respectively.
    EphB1-IN-1
  • HY-101820
    Simotinib
    		Inhibitor 99.39%
    Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
    Simotinib
  • HY-P990238
    Anti-Human/Rat HER2 (neu) Antibody (7.16.4)
    		Inhibitor
    Anti-Human/Rat HER2 (neu) Antibody (7.16.4) is an anti-mouse HER2 IgG2a monoclonal antibody. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) reduces tumor cell proliferation by inhibiting the HER2 signaling pathway. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) can activate CD8+ T cells. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) can be used for research on cancer such as breast cancer.
    Anti-Human/Rat HER2 (neu) Antibody (7.16.4)
  • HY-19803
    Naquotinib mesylate
    		Inhibitor 98.05%
    Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
    Naquotinib mesylate
  • HY-12029
    WZ8040
    		Inhibitor 99.22%
    WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal.
    WZ8040
  • HY-19816A
    Avitinib maleate
    		Inhibitor 99.86%
    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-18603
    FIIN-3
    		Inhibitor 99.66%
    FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
    FIIN-3
  • HY-107367A
    Epertinib hydrochloride
    		Inhibitor 98.15%
    Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity. Epertinib (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Epertinib hydrochloride
  • HY-107364
    MTX-211
    		Inhibitor 99.81%
    MTX-211 (Mol 211) is a dual inhibitor of EGFR and PI3K with IC50 values of ＜100 nM. MTX-211 can be used for the research of cancer and other diseases.
    MTX-211
  • HY-147941A
    MS9427 TFA
    		Degrader 98.38%
    MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer.
    MS9427 TFA
  • HY-147219A
    SIAIS164018 hydrochloride
    		Inhibitor 99.84%
    SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857).
    SIAIS164018 hydrochloride
  • HY-N6932
    Voacamine
    		99.64%
    Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits EGFR to exert oncogenic activity against colorectal cancer.
    Voacamine
  • HY-116437
    Selatinib
    		Inhibitor 98.56%
    Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects.
    Selatinib
  • HY-157581
    MS39
    		Degrader 99.89%
    MS39 (compound 6) is a PROTAC targeting EGFR. MS39 is composed of PROTAC target protein ligand N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-(piperazin-1-yl)propoxy)quinazolin-4-amine (HY-W109039) (red part), E3 ligase ligand (S,R,S)-AHPC (HY-125845) (blue part) and PROTAC Linker Undecanedioic acid (HY-W014125) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC-CO-C9-acid (HY-139345). MS39 reduces the expression of EGFR and downstream signaling in HCC-827 and H3255 cells. MS39 inhibits the proliferation of H3255 cells.
    MS39
  • HY-107459
    (E/Z)-AG490
    		Inhibitor 99.71%
    (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
    (E/Z)-AG490
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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