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 Controls
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EGFR Substrate
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EGFR Ligands
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ErbB2/HER2 Proteins
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ErbB3/HER3 Proteins
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EGFR Proteins
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ErbB4/HER4 Proteins
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EGFR Related Products (1280)
Related Products (1280)
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Recombinant Proteins (112)
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Antibodies (19)
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EGFR Isoform Comparison
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EGFR/HER2-IN-13
0 ImagesCat. No.: HY-161602CAS No.: 3034701-46-4EGFR/HER2-IN-13 (Compd 38) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-13 can be used for cancer research.
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EGFR/ErbB-2 inhibitor-1
0 ImagesCat. No.: HY-156639CAS No.: 1135150-79-6EGFR/ErbB-2 inhibitor-1 is a ErbB2/HER2 inhibitor.
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EGFR-IN-97
0 ImagesCat. No.: HY-157432CAS No.: 3020681-05-1EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFRL858R/T790M/C797S and Ba/F3-EGFRDel19/T790M/C797S cells, with IC50 values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFRL858R/T790M/C797S cells at the concentration of 0.8 μM.
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AST5902 mesylate
0 ImagesCat. No.: HY-138627BCAS No.: 2412155-75-8AST5902 mesylate is the active metabolite of Furmonertinib (HY-112870) with antitumor activity, and acts as a EGFR inhibitor. AST5902 mesylate inhibits CYP3A4 mRNA transcription at low concentrations and induces CYP3A4 mRNA expression at high concentrations. AST5902 mesylate can be used in research related to non-small cell lung cancer.
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ZNL-0056
0 ImagesCat. No.: HY-160564CAS No.: 2767987-38-0
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Lys-PEG3-BA
0 ImagesCat. No.: HY-180964CAS No.: 3057939-67-7Lys-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader with DC50 values of 1.32 and 19.66 μM for H3122 (EML4-ALK) and H1975 (EGFR-L858R/T790M) cells, respectively. Lys-PEG3-BA hinders proliferation via rewiring the ubiquitin- proteasome system in vitro. Lys-PEG3-BA can be used for non-small cell lung cancer research.
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EGFR/PARP-1-IN-1
0 ImagesCat. No.: HY-183373EGFR/PARP-1-IN-1 is a dual EGFR and PARP-1 inhibitor with IC50 values of 64 nM and 12 nM, respectively. EGFR/PARP-1-IN-1 binds to the ATP-binding pocket of EGFR and interacts with the catalytic domain of PARP-1, inhibiting kinase and enzymatic activity via hydrogen bond formation with key residues in both targets. EGFR/PARP-1-IN-1 induces apoptosis through the endogenous mitochondrial pathway, arrests the cell cycle at the G2 phase, and inhibits cell proliferation. EGFR/PARP-1-IN-1 can be used for research on triple-negative breast cancer.
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EGFR/BRAFV600E-IN-6
0 ImagesCat. No.: HY-180154CAS No.: 3120155-78-1EGFR/BRAFV600E-IN-6 (Compound 7c) is a dual EGFR/BRAFV600E inhibitor with IC50 values of 0.12 and 0.05 μM. EGFR/BRAFV600E-IN-6 can activate caspase-3/8/9, unregulate Bax expression and downregulate Bcl-2 levels. EGFR/BRAFV600E-IN-6 can induce apoptosis and shows antioxidant activity. EGFR/BRAFV600E-IN-6 can be used for the research of cancer, such as colon cancer.
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EGFR-IN-43
0 ImagesCat. No.: HY-145824CAS No.: 3031307-74-8EGFR-IN-43 (Compound 17c) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-43 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-43 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-43 has superior anti-cancer activity.
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EGFR/HER2-IN-6
0 ImagesCat. No.: HY-151156CAS No.: 2820126-50-7EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer.
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EGFR-IN-123
0 ImagesCat. No.: HY-162891CAS No.: 2543763-00-2EGFR-IN-123 (compound D06) is a potent EGFR inhibitor. EGFR-IN-123 inhibits PC-9G, A549, A431 and HCT116 cells with IC50s of 0.74, 1.36, 1.20 and 2.53 μM, respectively.
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EGFR/BRAFV600E-IN-1
0 ImagesCat. No.: HY-147825CAS No.: 2492429-45-3EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAFV600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively.
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Tyrphostin AG213
0 ImagesCat. No.: HY-101959CAS No.: 122520-86-9Synonyms: AG213Tyrphostin AG213 (AG213) is an inhibitor of epidermal growth factor receptor (EGFR) protein tyrosine kinase (IC50=0.85 μM). Tyrphostin AG213 inhibits tyrosine kinase activity IC50=2.4 μM) and topoisomerase II (IC100=50 μM). Tyrphostin AG213 can induce nonapoptotic cell programmed death in tumor cells.
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EGFR-IN-67
0 ImagesCat. No.: HY-147996CAS No.: 2416924-99-5EGFR-IN-67 (Compound 7d) is a potent EGFR inhibitor with an IC50 of 0.34 μM. EGFR-IN-67 shows anticancer activity.
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EGFR-IN-206
0 ImagesCat. No.: HY-182064EGFR-IN-206 is an orally active EGFR inhibitor. EGFR-IN-206 inhibits the phosphorylation of the key tumor growth protein EGFR, and suppresses the proliferation, migration and invasion of EGFR triple-mutant tumor cell lines. EGFR-IN-206 downregulates the expression of inflammation-related proteins iNOS, COX-2 and NF-κB (p65). EGFR-IN-206 promotes the secretion of NO. EGFR-IN-206 reduces the secretion of IL-6. EGFR-IN-206 induces apoptosis (apoptosis) of EGFR triple-mutant tumor cells. EGFR-IN-206 exerts antitumor activity in EGFR triple-mutant mice. EGFR-IN-206 is applicable to the research of non-small cell lung cancer.
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EGFR/VEGFR2-IN-13
0 ImagesCat. No.: HY-183090EGFR/VEGFR2-IN-13 is a multi-target inhibitor, with an IC50 of 0.98 µM against VEGFR-2, 1.01 µM against EGFR, and 1.94 µM against topoisomerase II. EGFR/VEGFR2-IN-13 induces cell cycle arrest and apoptosis in tumor cells. As an anticancer agent, EGFR/VEGFR2-IN-13 exhibits cytotoxicity against cancer cells. EGFR/VEGFR2-IN-13 can be used in research related to breast cancer, colon cancer, and liver cancer.
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EGFR-IN-181
0 ImagesCat. No.: HY-178939EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM). EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases.
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EG31
0 ImagesCat. No.: HY-172966CAS No.: 360760-58-3EG31 is an EGFR inhibitor. EG31 effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells (GI50 values of MDA-MB-231 and Hs578T cells are 498.90 nM and 740.73 nM, respectively) and induces apoptosis by inhibiting the EGFR signaling pathway. EG31 still maintains antiproliferative activity against 5-fluorouracil (5-FU)-resistant TNBC cells (GI50: 519.5 nM). EG31 can be used to study TNBC resistance.
