The epidermal growth factor receptor (EGFR; ErbB1) is a member of the epidermal growth factor RTK (receptor tyrosine kinases) family, which also includes HER2/neu (ErbB2), ErbB3 (HER3), and ErbB4 (HER4). The extracellular ligand-binding ectodomain, the single chain transmembrane domain, and the intracellular tyrosine kinase domain make up the EGFR, which is located at the cell surface. Epidermal growth factor (EGF), transforming growth factor (TGF-), amphiregulin, heparin-binding EGF, and betacellulin are just a few of the ligands that bind to and activate the EGFR.
The tyrosine kinase domain is activated by the receptors' formation of homo- or heterodimeric complexes after ligand binding. The Ras-Raf-MAP kinase, PI-3K/Akt, PKC, and Stat/Jak signaling pathways are all activated as a result of the dimerization and autophosphorylation of EGFR. The EGFR is activated to control cellular survival, differentiation, and proliferation. The EGFR has been derided as a proto-oncogene primarily because of its function in encouraging cell proliferation and preventing apoptosis.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
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V33525 | (E)-AG 99 (AG99) | 122520-85-8 | (E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor. |
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V0554 | AC480 (BMS599626) | 714971-09-2 | AC480 (also known as BMS-599626) is a novel, potent, orally bioavailable, selective and efficacious inhibitor of HER1/2 (human epidermal growth factor receptors) with potential anticancer activity. |
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V0504 | AEE788 (NVP-AEE788) | 497839-62-0 | AEE788 (NVP-AEE-788; NVP-AEE788) is a novel, potent and orally bioavailable inhibitor of multiple receptor tyrosine kinase such as EGFR (epidermal growth factor receptor) and HER2/ErbB2 with potential antitumor activity. |
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V0536 | Afatinib (BIBW2992) | 850140-72-6 | Afatinib (formerly BIBW 2992; BIBW-2992; brand name: Gilotrif), is a potent, covalent/irreversible, and orally bioavailable dual (EGFR/ErbB) receptor tyrosine kinase (RTK) inhibitor with anticancer activity. |
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V0542 | Afatinib (BIBW2992) Dimaleate | 850140-73-7 | Afatinib dimaleate (the maleate salt form of Afatinib, also know as BIBW-2992; BIBW2992) is a potent, covalent/irreversible,and orally bioavailable dual EGFR/HER2 receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. |
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V10440 | AG 30 (Tyrphostin AG30) | 122520-79-0 | An antimicrobial peptide with angiogenic properties, AG-30/5C, activates human mast cells through the MAPK and NF-κB pathways. |
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V0560 | AG-1478 (Tyrphostin AG-1478; NSC693255) | 153436-53-4 | AG-1478 (also known as Tyrphostin AG1478; AG-1478; NSC-693255) is a novel, potent and selective EGFR (epidermal growth factor receptor) inhibitor with potential antitumor and antidiabetic activity. |
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V3989 | AG-1557 | 189290-58-2 | AG-1557 is a novel and potent inhibitor of epidermal growth factor receptor tyrosine(EGFR)kinase. |
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V0549 | AG-18 (RG50858, TX-825) | 118409-57-7 | AG-18 (also known as RG-50810, RG-50858, TX 825, Tyrphostin A23 andTyrphostin AG-18) isa novel and potentEGFRinhibitor with anIC50andKi of 35 and 11 μM, respectively. |
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V7601 | AG555 | 133550-34-2 | AG 555 (Tyrphostin AG 555) is a potent antiretroviral active molecule and a potent and specific EGFR inhibitor that blocks Cdk2 activation. |
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V4747 | Alflutinib mesylate (Furmonertinib) | 2130958-55-1 | Alflutinib mesylate (formerly also known as AST-2818; AST2818; Furmonertinib), the mesylate salt form of Alflutinib, is a novel, irreversible and 3rd generation EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor (TKI) selective for EGFR T790M mutation. |
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V0561 | Allitinib (AST 1306) | 897383-62-9 | Allitinib (formerly also known as AST1306; AST-1306) is a novel, potent, selective and covalent / irreversible inhibitor of EGFR and ErbB2 with potential antitumor activity. |
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V37619 | Almonertinib (HS-10296) | 1899921-05-1 | Almonertinib (HS10296)is a novel, potent, orally bioavailable, 3rd-generation irreversible inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. |
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V30518 | AV-412 | 451492-95-8 | AV-412 free base (MP-412 free base) is an EGFR inhibitor. |
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V3696 | Avitinib (AC0010) | 1557267-42-1 | Avitinib (Abivertinib, AC-0010, AC-0010MA, AC0010, AC0010MA) is a pyrrolopyrimidine-based,orally bioactive, and irreversible/covalent inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with selectivity against T790M resistance mutations. |
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V0541 | AZ5104 | 1421373-98-9 | AZ5104 (AZ-5104), a demethylated and active metabolite of Osimertinib (AZD-9291), isanirreversible EGFRinhibitor with potential antitumor activity. |
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V3490 | BMS-690514 | 859853-30-8 | BMS-690514 is a novel, potent and orally bioavailable inhibitor of EGFR [human epidermal growth factor receptor (HER) 1] and VEGFR (vascular endothelial growth factor receptors) with IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively. |
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V0550 | Butein (NSC-652892; CCG208298; CS-5675; AC 1NQY7L) | 487-52-5 | Butein (NSC 652892; CCG-208298; CS5675; AC1NQY7L) is a naturally occuring plant polyphenol and chalconoid isolated from Rhus verniciflua with a broad spectrum of pharmacological effects such as antiinflammatory, antioxidative, aldose reductase and advanced glycation endproducts inhibitory and anticancer activities. |
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V0539 | Canertinib (CI-1033; PD-183805) | 267243-28-7 | Canertinib (formerly CI-1033; CI1033; PD183805; PD-183805) is anirreversible/covalent, quinazoline-based and orally bioavailable pan-ErbB inhibitor for EGFR and ErbB2 with potential antineoplastic activity. |
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V5745 | Canertinib HCl | 289499-45-2 | Canertinib (formerly also known as CI-1033; CI 1033; PD-183805) is a novel, potent and orally bioavailable quinazoline class of pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, respectively. |
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