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.
EGFR Isoform Specific Products
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EGFR Inhibitors
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EGFR Agonists
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EGFR Antagonists
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EGFR Activators
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EGFR Modulators
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EGFR Chemicals
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EGFR Inducers
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EGFR Degraders
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EGFR Substrate
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EGFR Ligands
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ErbB2/HER2 Proteins
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EGFR Proteins
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ErbB4/HER4 Proteins
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EGFR Related Products (1259)
Related Products (1259)
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Recombinant Proteins (110)
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Antibodies (19)
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EGFR Isoform Comparison
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Dacomitinib (Standard)
0 ImagesSynonyms: PF-00299804 (Standard); PF-299804 (Standard)Dacomitinib (Standard) is the analytical standard of Dacomitinib. This product is intended for research and analytical applications. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
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Erlotinib mesylate
0 ImagesCat. No.: HY-12008ACAS No.: 248594-19-6Synonyms: CP-358774 mesylate; NSC 718781 mesylate; OSI-774 mesylateErlotinib (CP-358774) mesylate is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib mesylate also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib mesylate blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib mesylate inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib mesylate is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib mesylate can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis.
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Canertinib (Standard)
0 ImagesSynonyms: CI-1033 (Standard); PD-183805 (Standard)Canertinib (Standard) is the analytical standard of Canertinib. This product is intended for research and analytical applications. Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice.
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Rociletinib hydrobromide (Standard)
0 ImagesSynonyms: CO-1686 hydrobromide (Standard); AVL-301 hydrobromide (Standard); CNX-419 hydrobromide (Standard)Rociletinib hydrobromide (Standard) is the analytical standard of Rociletinib hydrobromide. This product is intended for research and analytical applications. Rociletinib hydrobromide (CO-1686 hydrobromide) 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.
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AKOS024836912
0 ImagesCat. No.: HY-137081CAS No.: 1705763-81-0AKOS024836912 is a EGFR-EGF interaction inhibitor. AKOS024836912 is applicable to research related to non-small cell lung cancer.
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Icotinib (Standard)
0 ImagesCat. No.: HY-15164ARCAS No.: 610798-31-7Synonyms: BPI-2009 (Standard)Icotinib (Standard) is the analytical standard of Icotinib. This product is intended for research and analytical applications. Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M and EGFRL861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Tyrphostin 23 (Standard)
0 ImagesCat. No.: HY-15644RCAS No.: 118409-57-7Synonyms: Tyrphostin A23 (Standard); RG-50810 (Standard); AG 18 (Standard)Tyrphostin 23 (Standard) is the analytical standard of Tyrphostin 23. This product is intended for research and analytical applications. Tyrphostin 23 (Tyrphostin A23) is an EGFR inhibitor with an IC50 and Kiof 35 and 11 μM, respectively.
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Eucommin A
0 ImagesCat. No.: HY-N20729CAS No.: 99633-12-2
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ZM-306416 hydrochloride
0 ImagesCat. No.: HY-110045CAS No.: 196603-47-1ZM-306416 (CB-676475) hydrochloride is a potent VEGFR inhibitor with IC50s of 0.1 μM and 2 μM for KDR and Flt, respectively. ZM-306416 hydrochloride is also a EGFR inhibitor with an IC50 of <10 nM.
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Paeciloquinone C
0 ImagesCat. No.: HY-N14637CAS No.: 92439-42-4Paeciloquinone C can inhibit the EGFR protein tyrosine kinase. Paeciloquinone C inhibits the V-abl protein tyrosine Kinase with an IC50 of 0.56 μM.
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MTX-211 (Standard)
0 ImagesCat. No.: HY-107364RCAS No.: 1952236-05-3Synonyms: Mol 211 (Standard)MTX-211 (Standard) (Mol 211 (Standard)) is the analytical standard of MTX-211 (HY-107364). This product is intended for research and analytical applications. 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.
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TX1-85-1 (Standard)
0 ImagesCat. No.: HY-100848RCAS No.: 1603845-32-4TX1-85-1 (Standard) is the analytical standard of TX1-85-1 (HY-100848). This product is intended for research and analytical applications. TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.
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1,2,3,4-Tetrahydro Staurosporin
0 ImagesCat. No.: HY-W740378CAS No.: 220038-19-7Synonyms: AFN-9411,2,3,4-Tetrahydrostaurosporine is a derivative of Staurosporine (HY-15141) and an inhibitor of mutant EGFR (IC50=74 nM for EGFRT790M). It is selective for EGFRT790M over wild-type EGFR (IC50=390 nM). It also binds to Janus kinase 3 (JAK3).
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Rezivertinib (Standard)
0 ImagesCat. No.: HY-109189RCAS No.: 1835667-12-3Synonyms: BPI-7711 (Standard)Rezivertinib (Standard) is the analytical standard of Rezivertinib (HY-109189). This product is intended for research and analytical applications. Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine Kinase inhibitor (TKi). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
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Pelitinib (Standard)
0 ImagesSynonyms: EKB-569 (Standard); WAY-EKB 569 (Standard)Pelitinib (Standard) is the analytical standard of Pelitinib. This product is intended for research and analytical applications. 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.
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HKI-357 (Standard)
0 ImagesCat. No.: HY-103443RCAS No.: 848133-17-5HKI-357 (Standard) is the analytical standard of HKI-357 (HY-103443). This product is intended for research and analytical applications. HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
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CNBDA
0 ImagesCat. No.: HY-156487CAS No.: 2101321-90-6CNBDA is a selective SHP2 inhibitor with an IC50 of 5 μM. CNBDA binds to the active site of SHP2 through interactions with surrounding positively charged and polar amino acids, inhibits the PTPase activity of SHP2, and blocks the autodephosphorylation of SHP2. CNBDA inhibits the transformed phenotype, proliferation, anchorage-independent growth, and mammosphere formation of breast cancer cells, as well as EGF-induced Ras-ERK and PI3K-Akt signaling pathways, downregulates HER2 expression, and induces cell death. CNBDA can be used in breast cancer-related research.
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BMS-690514 (Standard)
0 ImagesCat. No.: HY-10333RCAS No.: 859853-30-8BMS-690514 (Standard) is the analytical standard of BMS-690514 (HY-10333). This product is intended for research and analytical applications. BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.
