The receptor tyrosine kinase family of the epidermal growth factor, which also includes HER2/neu (ErbB2), ErbB3 (HER3), and ErbB4 (HER4), includes the epidermal growth factor receptor (EGFR; ErbB1). 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 |
---|---|---|---|---|
V2023 | Nazartinib mesylate (EGF81) | 1508250-72-3 | Nazartinib mesylate (formerly known as EGF816 mesylate and NVS-816 mesylate) is a novel, covalent/irreversible, and mutant-selective EGFR inhibitor with Kiand Kinactof 31 nM and 0.222 min−1on EGFR(L858R/790M) mutant, respectively. | |
V2697 | Nazartinib S-enantiomer (EGF816) | 1508256-20-9 | Nazartinib S-enantiomer is the S-isomer of Nazartinib which is a novel, covalent/irreversible, mutant-selective EGFR inhibitor with Kiand Kinactof 31 nM and 0.222 min−1on EGFR(L858R/790M) mutant, respectively. | |
V69397 | Neratinib-d6 (neratinib d6) | 1259519-18-0 | Neratinib-d6 is the deuterated form of neratinib. | |
V69366 | Nezutatug | 2673271-78-6 | Nezutatug is an anti-HER3 antibody used in cancer-related research. | |
V69332 | Nimotuzumab | 780758-10-3 | Nimotuzumab is a humanized IgG1 monoclonal antibody (mAb) targeting EGFR with a KD of 0.21 nM. | |
V2675 | NSC228155 | 113104-25-9 | NSC228155 is a novel and potent activator of EGFR, which binds to the sEGFR dimerization domain II and modulate EGFR tyrosine phosphorylation. | |
V18421 | Olafertinib | 1660963-42-7 | Olafertinib, formerly known as CK-101 and Olafertinib, is a potent and orally bioavailable EGFR mutant-specific inhibitor. | |
V81005 | Oligopeptide-41 | Oligopeptide-41 is a biologically active peptide with hair growth-promoting effects that has been reported for use as an ingredient of cosmetics. | ||
V4484 | Olmutinib | 1353550-13-6 | Olmutinib (also known as HM61713 and BI-1482694; Olita) is a novel, potent, orally bioavailable, third-generation and irreversible EFGR/epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI). | |
V69403 | Oritinib (SH-1028) | 2035089-28-0 | SH-1028 is an irreversible third-generation EGFR TKI that can overcome T790M-mediated drug resistance in non-small cell lung cancer. | |
V69416 | Oritinib mesylate (SH-1028 mesylate) | 2180164-79-6 | Oritinib (SH-1028) mesylate is a selective, orally bioactive, pyrimidine-based irreversible EGFR inhibitor. | |
V81015 | Os30 | Os30 is a potent fourth-generation EGFR inhibitor and a potent EGFRC797S-TK inhibitor (antagonist) with IC50s of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. | ||
V69340 | Osimertinib-d6 (AZD-9291-d6; Mereletinib-d6) | 1638281-44-3 | Osimertinib-d6 is deuterium-labeled Osimtinib. | |
V3248 | PD153035 | 153436-54-5 | PD153035 is reported to be a novel, potent, specific, andATP competitive inhibitor of EGFR (Epidermal growth factor receptor) tyrosine kinase with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays, and to a lesser degree, of the closely related HER2/neu receptor; PD153035 inhibits EGF-dependent EGFR phosphorylation in a variety of human cancer cell lines over-expressing EGFRs, which include A431, Difi, DU145, MDA-MB-468, ME180 and C4i, with IC50 of 0.22 μM, 0.3 μM, 0.4 μM, 0.68 μM, 0.95 μM and 2.5 μM respectively. | |
V69402 | Petosemtamab (MCLA 158) | 2213450-26-9 | Petosemtamab (MCLA 158) is an anti-EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). | |
V4473 | PF-06459988 | 1428774-45-1 | PF-06459988 (PF06459988) is an orally bioavailable, 3rd-generation, covalent/irreversible inhibitor of T790M-Containing EGFR Mutants with potential anticancer activity. | |
V69361 | Pimurutamab | 2251771-76-1 | Pimurutamab is a humanized IgG1-κ antibody targeting EGFR. | |
V69390 | PKI-166 hydrochloride | 2230253-82-2 | PKI-166 HCl is a highly efficient, selective, orally bioavailable EGFR tyrosine kinase inhibitor (TKI) (antagonist) with IC50 of 0.7 nM. | |
V69343 | Ponezumab (PF-04360365; RN 1219) | 1178862-65-1 | Ponezumab (PF-04360365) is a humanized anti-amyloid IgG2 monoclonal antibody (mAb). | |
V69387 | pp60 (v-SRC) Autophosphorylation Site, Phosphorylated | 176042-83-4 | pp60 (v-SRC) Autophosphorylation Site, Phosphorylate is a phosphorylated short peptide of EGFR substrate. |