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 Proteins
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EGFR Related Products (1295)
Related Products (1295)
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Recombinant Proteins (112)
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Antibodies (19)
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EGFR Isoform Comparison
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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.: 99633-12-2Eucommin A is a natural polyphenolic antioxidant. Eucommin A forms stable complexes with EGFR and MAPK8 via hydrogen bonding and hydrophobic interactions, and regulates osteoarthritis-related Autophagy. Eucommin A is applicable to research related to oxidative stress, such as osteoarthritis.
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ZM-306416 hydrochloride
0 ImagesCat. No.: HY-110045CAS No.: 196603-47-1
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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.
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Erlotinib-d4
0 ImagesCat. No.: HY-50896S2CAS No.: 1130852-41-3Synonyms: CP-358774-d4; NSC 718781-d4; OSI-774-d4Erlotinib-d4 (CP-358774-d4) is the deuterated-labeled Erlotinib (HY-50896). 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, fibronectin, α-SMA, collagen deposition, 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, pancreatic cancer, renal fibrosis, and other conditions.
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4(3H)-Quinazolinone (Standard)
0 Images4(3H) -quinazolinone is a fused nitrogen heterocyclic compound whose derivatives have a wide range of antimicrobial and antitumor activities.
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G3130
0 ImagesCat. No.: HY-111300CAS No.: 848952-37-4G3130 is a reversible HSP90 inhibitor with a Kd value of 280 nM for the N-terminal ATP-binding domain of purified human Hsp90α. G3130 binds to the adenine site via a multi-hydrogen bond network. G3130 induces the degradation of Hsp90 client protein Her-2 in breast cancer cells. G3130 activates Hsp70 promoter-driven luciferase expression in 293T cells. G3130 can be used in breast cancer-related research.
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Lapatinib-d7
0 ImagesCat. No.: HY-50898S4CAS No.: 1009307-23-6Synonyms: GW572016-d7; GW2016-d7
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Trastuzumab envedotin
0 ImagesCat. No.: HY-172820Synonyms: DP303cTrastuzumab envedotin (DP303c) is a anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab envedotin is composed of the tubulin polymerization inhibitor Monomethyl auristatin E (MMAE) (HY-15162) to the anti-HER2 antibody DP001 via a cleavable linker. Trastuzumab envedotin can be used for the research of HER2-positive solid tumors, such as breast cancer, colorectal cancer, and gastric cancer.
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LDC8201
0 ImagesCat. No.: HY-184315CAS No.: 2411873-31-7LDC8201 is a selective, orally active, covalent inhibitor that targets EGFR and Her2 exon 20 insertion mutants. LDC8201 induces tumor shrinkage and regression. LDC8201 is applicable to research related to non-small cell lung cancer carrying EGFR or Her2 exon 20 insertion mutations.
