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-155537
    Pruvonertinib
    		Inhibitor 99.50%
    YK-029A is an orally active inhibitor of mutant EGFR，targeting to both the T790M mutations (EGFRT790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity，and results tumor regression in EGFRex20ins-driven PDX models.
    Pruvonertinib
  • HY-150611
    EGFR-IN-70
    		Inhibitor 99.16%
    EGFR-IN-70 (compound 18j) is a potent EGFR inhibitor with IC50 values of 23.6 and 307.5 nM for EGFRLR/TM/CS and EGFRWT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research.
    EGFR-IN-70
  • HY-10261B
    (E/Z)-Afatinib
    		Inhibitor 99.98%
    (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.
    (E/Z)-Afatinib
  • HY-101219
    VEGFR-IN-1
    		Inhibitor 98.42%
    VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively.
    VEGFR-IN-1
  • HY-164702
    BL-B01D1
    		Inhibitor 99.53%
    BL-B01D1 is a bispecific ADC, which targets EGFR and HER3 through bispecific antibody Izalontamab (HY-P99676), and exhibits cytotoxicity against various cancer cells via inhibition of DNA replication and DNA synthesis by its ADC toxin ED04 (HY-153891).
    BL-B01D1
  • HY-103442
    CGP52411
    		Inhibitor 99.82%
    CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
    CGP52411
  • HY-18963
    Lavendustin A
    		Inhibitor 98.95%
    Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis.
    Lavendustin A
  • HY-N7005
    Clitorin
    		Inhibitor 99.45%
    Clitorin is an orally active flavonoid compound that can be isolated from Carica papaya. Clitorin is an inhibitor of EGFR (IC50: 89.58 nM) and aromatase (IC50: 77.41 nM). Clitorin has antioxidant and anti-tumor activities. In the DPPH and ABTS radical scavenging assays, Clitorin has IC50 values of 91.96 ppm and 250.45 ppm, respectively. In addition, Clitorin can regulate lipogenesis and fatty acid oxidation and can be used in the research of non-alcoholic fatty liver disease.
    Clitorin
  • HY-19729
    Naquotinib
    		Inhibitor 98.71%
    Naquotinib (ASP8273) 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
  • 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-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-128576
    DS21360717
    		99.80%
    DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC50 of 0.49 nM. Anti-cancer activity.
    DS21360717
  • HY-139920
    Oritinib
    		Inhibitor 99.59%
    Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFRWT, EGFRL858R, EGFRL861Q, EGFRL858R/T790M, EGFRd746-750 and EGFRd746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.
    Oritinib
  • HY-118263
    Dacomitinib hydrate
    		Inhibitor 99.03%
    Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC).
    Dacomitinib hydrate
  • 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-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 99.66%
    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-156640
    Rocbrutinib
    		Inhibitor 99.76%
    Rocbrutinib is a Bruton's tyrosine kinase inhibitor with antineoplastic effect.
    Rocbrutinib
  • HY-116437
    Selatinib
    		Inhibitor 99.83%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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