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 |
---|---|---|---|---|
V69436 | EGFR-IN-62 | 2890261-65-9 | EGFR-IN-62 (compound 9h) is a potent EGFR kinase inhibitor (antagonist) with IC50s of 10 nM (L858R/T790 M), 29 nM (WT) and 242 nM (L858R/T790 M/C797S). | |
V69344 | EGFR-IN-70 | 2926716-96-1 | EGFR-IN-70 (compound 18j) is a potent EGFR inhibitor (antagonist) with IC50s of 23.6 and 307.5 nM for EGFRLR/TM/CS and EGFRWT, respectively. | |
V69421 | EGFR-IN-73 | 2857033-34-0 | EGFR-IN-73 (Compound 3f) is a potent inhibitor of EGFR Del19, the most common EGFR mutation, with IC50 of 119 nM. | |
V79266 | EGFR-IN-74 | EGFR-IN-74 (Compound 21) is a potent EGFR inhibitor (antagonist) with IC50 of 138 nM against EGFR L858R/T790M. | ||
V80366 | EGFR-IN-75 | EGFR-IN-75 is an inhibitor (blocker/antagonist) of EGFRWT and EGFRT790M with IC50s of 0.28 μM and 5.02 μM, respectively. | ||
V79152 | EGFR-IN-78 | EGFR-IN-78 (compound A5) is a 2-aminopyrimidine analogue, a reversible inhibitor of EGFRC797S-TK, and an inducer of apoptosis. | ||
V79267 | EGFR-IN-79 | EGFR-IN-79 (compound 21) is an EGFR inhibitor (antagonist) with anti-tumor activity. | ||
V69422 | EGFR-IN-80 | 171745-13-4 | EGFR-IN-80 (compound 30) is an EGFR inhibitor (antagonist) with pIC50 of 10.6. | |
V79268 | EGFR-IN-81 | EGFR-IN-81 (Compound 10i) is an EGFR inhibitor. | ||
V69391 | EGFR-IN-82 | 2568086-81-5 | EGFR-IN-82 (Cmpound 8a) is an orally bioactive EGFR inhibitor (antagonist) with IC50s of 0.09 and 0.06 nM for EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S, respectively, but has no obvious effect on EGFRWT. | |
V79490 | EGFR-IN-83 | EGFR-IN-83 (Compound 9) is an EGFR inhibitor (IC50= 2.53 nM). | ||
V79269 | EGFR-IN-84 | EGFR-IN-84 (Compound 6g) is an EGFR inhibitor (IC50= 24 nM). | ||
V69353 | EGFR-IN-85 | 1956378-29-2 | EGFR-IN-85 (Compound 1) is an EGFR inhibitor. | |
V79925 | EGFR-IN-86 | EGFR-IN-86 (compound 4i) is an EGFR inhibitor (IC50= 1.5 nM) with high activity against glioblastoma. | ||
V69377 | EGFR-IN-87 | 1835666-87-9 | EGFR-IN-87 is an EGFR tyrosine kinase inhibitor. | |
V69418 | EGFR-IN-89 | 2413029-40-8 | EGFR-IN-89 (compound 13k) is a potent fourth-generation EGFR mutation inhibitor (antagonist) with IC50 of 10.1 nM against Del19/T790M/C797S mutation. | |
V69431 | EGFR-IN-9 | 1226549-39-8 | EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor (antagonist) with IC50s of 7 nM and 28 nM for wild-type EGFR kinase and double mutant EGFR kinase (L858R/T790M), respectively. | |
V79270 | EGFR-IN-90 | EGFR-IN-90 (compound 34) is an orally bioactive EGFR inhibitor. | ||
V79399 | EGFR-IN-91 | EGFR-IN-91 (compound 9) is an orally bioavailable EGFR inhibitor that can penetrate the BBB (blood-brain barrier). | ||
V69432 | EGFR/BRAF-IN-1 | 2906174-89-6 | EGFR/BRAF-IN-1 (compound 21) is a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione analogue, a potent EGFR/BRAF inhibitor, with IC50 of BRAFV600E is 45 nM. |