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 (1279)
Related Products (1279)
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Recombinant Proteins (112)
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Antibodies (19)
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EGFR Isoform Comparison
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Almonertinib hydrochloride
0 ImagesSynonyms: HS-10296 hydrochlorideAlmonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer.
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Rezivertinib
0 ImagesSynonyms: BPI-7711Rezivertinib (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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FSK hydrochloride
0 ImagesFSK hydrochloride is fluorosulfonyloxybenzoyl-L-lysine, which features a long, flexible aryl fluorosulfate-containing side chain that can reach protein sites inaccessible to covalent conjugation. FSK hydrochloride modifies nanomolecules to target epidermal growth factor receptor (EGFR), resulting in irreversibly bound covalent interactions. Through genetically encoded chemical crosslinking, FSK hydrochloride captures unknown enzyme-substrate interactions in living cells, targets residues other than Cys, and mediates crosslinking at the binding periphery. FSK hydrochloride enables the construction of a bioreactive SuFEx system for generating covalent bonds in various proteins both in vitro and in vivo.
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PD-161570
0 ImagesPD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
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SJF-1528
0 ImagesSJF-1528 (PROTAC 1) is a potent EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutant EGFR in HeLa cells. SJF-1528 also degrades HER2. SJF-1528 promotes ubiquitination and degradation of EGFR and can be used in breast cancer research.
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Mobocertinib succinate
0 ImagesSynonyms: TAK-788 succinate; AP32788 succinateMobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research.
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MS154
0 ImagesMS154 is a first-in-class E3 ligase cereblon-recruited EGFR degrader with Kd values of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutant, respectively. MS154 potently induces degradation of mutant, but not wild-type, EGFR in cancer cell lines in an E3 ligase-dependent manner. MS154 exhibits anticancer effects against lung cancer (blue: E3 ligase ligand (HY-103596); black: linker (HY-W096167); pink: EGFR ligand (HY-168305)).
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limertinib
0 ImagesSynonyms: ASK120067limertinib (ASK120067) is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC).
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Befotertinib
0 ImagesSynonyms: D-0316Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFRT790M, EGFRL858R and delE746-A750, forms covalent bonds with EGFRC797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib can be used in research related to multidrug-resistant cancers and non-small cell lung cancer.
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Becotatug
0 ImagesSynonyms: JMT-101; MRG003 AntibodyBecotatug (JMT-101) is a humanized IgG1 monoclonal antibody targeting epidermal growth factor receptor (EGFR), and serves as the antibody component of the antibody-drug conjugate Becotatug vedotin (HY-171265). Becotatug specifically binds to the extracellular domain of EGFR, induces receptor internalization and degradation, blocks the EGFR signaling pathway, and mediates antibody-dependent cellular cytotoxicity. When conjugated to monomethyl auristatin E (MMAE) (HY-15162) via a valine-citrulline cleavable linker, Becotatug enables targeted delivery of cytotoxic drugs to EGFR-positive tumor cells. Becotatug can be used for research related to non-small cell lung cancer, nasopharyngeal carcinoma, and head and neck squamous cell carcinoma..
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Ficerafusp alfa
0 ImagesSynonyms: BCA-101; FMAB2Ficerafusp alfa (BCA-101) is a bispecific antibody targeting EGFR and TGFβ, with a Kd of 2.58 nM against EGFR and a Kd of 61.3 nM against TGFβ1. Ficerafusp alfa binds to EGFR, inhibits EGFR phosphorylation, blocks EGF-dependent cell proliferation, and mediates antibody-dependent cellular cytotoxicity against EGFR-positive tumor cells. Ficerafusp alfa sequesters TGFβ via its TGFβRII ECD domain, neutralizes the activity of TGFβ and TGFβ1, and blocks TGFβ-dependent processes, including epithelial-mesenchymal transition, cell invasion, and differentiation of inducible regulatory T cells. Ficerafusp alfa is applicable to research related to head and neck squamous cell carcinoma, advanced solid tumors, squamous non-small cell lung cancer, anal squamous cell carcinoma, colorectal cancer, and pancreatic cancer.
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p-SCN-Bn-NOTA trihydrochloride
0 Imagesp-SCN-Bn-NOTA trihydrochloride is a macrocyclic chelator. p-SCN-Bn-NOTA trihydrochloride can be covalently coupled to molecules such as peptides through the thiocyanate group to form hexacoordinate copper (such as 64Cu) complexes. p-SCN-Bn-NOTA trihydrochloride specifically binds to GRPR or EGFR highly expressed on the surface of tumor cells, mediating tumor enrichment of radioactive probes. p-SCN-Bn-NOTA trihydrochloride can be used to study malignant tumors expressing GRPR or EGFR, such as prostate cancer and colorectal cancer.
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MAPK-IN-2
0 ImagesMAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFRT790M IC50=69 nM and B-RAFV600E IC50=83 nM).
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Erlotinib (Standard)
0 ImagesSynonyms: CP-358774 (Standard); NSC 718781 (Standard); OSI-774 (Standard)Erlotinib Standard (CP-358774 Standard) is the analytical standard of Erlotinib (HY-50896). This product is intended for research and analytical applications. Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib 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 blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib 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 is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib 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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EGA
0 ImagesEGA is an inhibitor that selectively targets the endosomal trafficking pathways. EGA targets the proteins involved in the endosomal trafficking pathways through which multiple toxins and viruses enter cells. EGA exerts its activity by inhibiting the trafficking from early endosomes to late endosomes, blocking the entry of multiple acid-dependent bacterial toxins and viruses into mammalian cells and delaying the lysosomal targeting and degradation of EGFR.
