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 (1284)
Related Products (1284)
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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 L718Q Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70706EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L718Q Recombinant Human Active Protein Kinase is a recombinant EGFR L718Q protein that can be used to study EGFR L718Q-related functions.
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KRAS G12D inhibitor 25
0 ImagesCat. No.: HY-168577CAS No.: 2768099-61-0KRAS G12D inhibitor 25 (Compound 148) is an inhibitor for KRAS G12C and HSP90α with IC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 inhibits the proliferation of MIA PaCa-2 and NCI-H358 with EC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 degrades ERBB2 with a DC50 of 0.1-1 μM.
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EGFR/VEGFR2-IN-11
0 ImagesCat. No.: HY-181766EGFR/VEGFR2-IN-11 is an EGFR/VEGFR2 inhibitor with IC50 values of 0.62 μM (human EGFR), 2.26 μM (human VEGFR-2), 17.38 μM (human COX-2), and 19.31 μM (human tubulin). EGFR/VEGFR2-IN-11 inhibits COX-2 activity and tubulin polymerization. EGFR/VEGFR2-IN-11 induces cell cycle arrest and apoptosis. EGFR/VEGFR2-IN-11 exerts selective and antiproliferative activity against human cancer cells. EGFR/VEGFR2-IN-11 can be used for the research of colon carcinoma, breast carcinoma, leukemia, lymphoma, glioblastoma.
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EGFR-IN-113
0 ImagesCat. No.: HY-158969CAS No.: 2549192-10-9EGFR-IN-113 (compound II-1) is an EGFR kinase inhibitor with an IC50 of 14.79 μM. EGFR-IN-113 can induce apoptosis and inhibit cell proliferation by downregulating Akt and Erk1/2 signaling. EGFR-IN-113 can be used for research in EGFR-driven cancers, such as lung cancer, pancreatic cancer, and breast cancer.
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EGFR-IN-60
0 ImagesCat. No.: HY-147826CAS No.: 2699877-43-3EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFRWT, EGFRT790M, EGFRL858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFRT790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFRWT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio.
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Cyclic(YCDGFYACYMDV)
0 ImagesCat. No.: HY-P10793CAS No.: 535959-77-4Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model.
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Topoisomerase II/EGFR-IN-1
0 ImagesCat. No.: HY-157402Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer.
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EGFR-IN-171
0 ImagesCat. No.: HY-175608EGFR-IN-171 is an EGFR inhibitor with an IC50 value of 0.19 μM. EGFR-IN-171 also inhibits vascular endothelial growth factor 2 (VEGFR-2) with an IC50 value of 31.65 μM. EGFR-IN-171 can induce apoptosis and G2/M phase cell cycle arrest. EGFR-IN-171 can be used for cancer research, such as liver and breast cancer.
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I-0436650
0 ImagesCat. No.: HY-189075CAS No.: 2843690-50-4I-0436650 is an orally active SHP2 inhibitor with an IC50 of 4 nM and a Kd value of 0.3 nM. I-0436650 binds allosterically to the channel between the C-SH2, N-SH2 and PTP catalytic domains, locking the protein in an inactive closed conformation. I-0436650 potently inhibits ERK phosphorylation and suppresses MAPK pathway activity. I-0436650 exhibits antiproliferative activity in EGFR- and RAS-dependent cells. I-0436650 can be used in the research of RAS-driven cancers, EGFR-mutated cancers and RTK-driven cancers.
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Sapitinib fumarate
0 ImagesCat. No.: HY-13050ACAS No.: 1196531-39-1Synonyms: AZD-8931 fumarate
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JGK-068S
0 ImagesCat. No.: HY-153744CAS No.: 2490431-16-6JGK-068S (compound I) is a potent EGFR inhibitor.
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Theophylline-platinum(IV) prodrug-1
0 ImagesCat. No.: HY-175257Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer.
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EGFR-IN-178
0 ImagesCat. No.: HY-178448EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC).
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EGFR T790M/L858R-IN-4
0 ImagesCat. No.: HY-158175CAS No.: 3032760-34-9
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EGFR/Akt/STAT3-IN-1
0 ImagesCat. No.: HY-189464EGFR/Akt/STAT3-IN-1 is an EGFR/Akt/STAT3 inhibitor (IC50 values of 9.79 μM, 17.80 μM, and 8.30 μM, respectively) that induces apoptosis and G0/G1 cell cycle arrest by inhibiting EGFR tyrosine kinase, Akt kinase, and STAT3 transcriptional activity, and exhibits selective cytotoxicity against cancer cells. EGFR/Akt/STAT3-IN-1 can be used for research on non-small cell lung cancer.
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EGFR-IN-156
0 ImagesCat. No.: HY-173492EGFR-IN-156 (Compound 7f) is an EGFR inhibitor that also has inhibitory activity against mutations EGFRL858R and EGFRT790M (IC50 values are 0.186, 0.131, and 0.107 μM, respectively). EGFR-IN-156 has significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer) (IC50 values are 1.67, 5.32, and 6.56 μM, respectively). EGFR-IN-156 inhibits cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. EGFR-IN-156 shows promise in EGFR-related cancers.
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EGFR-IN-62
0 ImagesCat. No.: HY-147862CAS No.: 2890261-65-9EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines.
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PROTAC EGFR degrader 16
0 ImagesCat. No.: HY-178242CAS No.: 2654821-07-3PROTAC EGFR degrader 16 is a selective EGFR PROTAC degrader with a DC50 value of < 50 nM. PROTAC EGFR degrader 16 can be used for the study of EGFR-driven cancerssuch as non-small cell lung cancer.
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EGFR/VEGFR2-IN-10
0 ImagesCat. No.: HY-179485EGFR/VEGFR2-IN-10 is a selective EGFR, VEGFR2 and COX2 inhibitor with IC50s of 8.5, 68 and 158 nM, respectively. EGFR/VEGFR2-IN-10 induces G1-phase cell cycle arrest in MCF-7 cells. EGFR/VEGFR2-IN-10 increases the Bax/Bcl-2 ratio, upregulates caspase-8, and elevates caspase-9 protein levels, confirming activation of the intrinsic apoptotic pathway. EGFR/VEGFR2-IN-10 demonstrates exceptional therapeutic potential by simultaneously inhibiting tumor proliferation, angiogenesis, and inflammation pathways while maintaining a favorable selectivity profile. EGFR/VEGFR2-IN-10 can be used as a research tool for cervical, liver, colon, and breast cancer studies.
