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 |
---|---|---|---|---|
V37821 | JBJ-04-125-02 R-isomer | 2060610-53-7 | JBJ-04-125-02 R-isomer, the R-enantiomer ofJBJ-04-125-02, is a novel, highly potent, mutant-specific, allosteric and orally bioavailable EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. | |
V69406 | JBJ-09-063 | 2820336-67-0 | JBJ-09-063 is a mutation-selective allosteric EGFR inhibitor (antagonist) with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S respectively. | |
V76864 | JBJ-09-063 hydrochloride | JBJ-09-063 HCl is a mutation-selective allosteric EGFR inhibitor (antagonist) with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S respectively. | ||
V76863 | JBJ-09-063 TFA | JBJ-09-063 TFA is a mutation-selective allosteric EGFR inhibitor (antagonist) with IC50 of 0.147 nM, 0.063 nM, 0.083 nM and EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S respectively. | ||
V69339 | JCN037 (JGK037) | 2305154-31-6 | JCN037 (JGK037) is a potent, covalent, BBB (blood-brain barrier) permeable (penetrable) EGFR inhibitor (antagonist) with IC50s of 2.49 nM, 3.95 nM and 4.48 nM for EGFR, p-wtEGFR and pEGFRvIII respectively. | |
V69426 | JGK-068S | 2490431-16-6 | JGK-068S (compound I) is a potent EGFR inhibitor. | |
V69433 | JNJ28871063 hydrochloride | 944342-90-9 | JNJ28871063 HCl is an orally bioactive, selective and ATP-competitive pan-ErbB kinase inhibitor (antagonist) with IC50s of 22 nM, 38 nM and 21 nM for ErbB1, ErbB2 and ErbB4 respectively. | |
V69347 | Laprituximab (J2898A) | 1622327-38-1 | Laprituximab (J2898A) is a humanized IgG1 anti-EGFR antibody that may be utilized to prepare the ADC IMGN289. | |
V69411 | Larotinib | 1438072-11-7 | Larotinib is a potent, broad-spectrum, orally bioactive tyrosine kinase inhibitor (TKI) with EGFR as its primary target, with IC50 of 0.6 nM. | |
V69405 | larotinib mesylate hydrate | 2097129-93-4 | Larotinib mesylate hydrate is a potent, broad-spectrum, orally bioactive tyrosine kinase inhibitor (TKI) with EGFR as the main target, with IC50 of 0.6 nM. | |
V23069 | Lavendustin A | 125697-92-9 | Lavendustin A, formerly known as RG 14355, is a potent, cell-permeable inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 11 nM). | |
V69352 | Losatuxizumab (ABT-806) | 1801544-27-3 | Losatuxizumab (ABT-806) is an anti-EGFR monoclonal antibody (mAb). | |
V69443 | Lumretuzumab (Anti-Human ERBB3 Recombinant Antibody) | 1448327-63-6 | Lumretuzumab (Anti-Human ERBB3 Recombinant Antibody) is a humanized anti-HER3 (ERBB3) monoclonal antibody (mAb) for use in cancer-related research. | |
V79896 | MAPK-IN-2 | MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor (antagonist) with anti-tumor activity. | ||
V5224 | MTX-211 | 1952236-05-3 | MTX-211 is a novel and potent dual inhibitor of EGFR and PI3K with the potential to be used for the treatment of cancer, in particular KRAS mutant colorectal cancer. | |
V80854 | MTX-241F | MTX-241F is a selective small molecule inhibitor targeting EGFR and PI3 kinase family members. | ||
V79895 | Multi-target kinase inhibitor 2 | Multi-target kinase inhibitor 2 (compound 5K) is a multi-targeted kinase inhibitor (antagonist) with the activity of inhibiting EGFR, Her2, VEGFR2 and CDK2 enzymes. | ||
V69368 | N-Desmethyl dosimertinib-d5 | 2719691-00-4 | N-Desmethyl dosimertinib-d5 is the deuterated form of dosimertinib. | |
V69374 | N-Methyl-dosimertinib-d5 | 2719690-98-7 | N-Methyl-dosimertinib-d5 is the deuterated form of dosimertinib. | |
V26243 | Naquotinib mesylate | 1448237-05-5 | Naquotinib mesylate (ASP-8273; ASP8273), the mesylate salt ofNaquotinib, is anirreversible/covalent and third-generation epidermal growth factor receptor (EGFR) inhibitor with potential anticancer activity. |