EGFR

EGFR

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.

EGFR related products

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.
Contact Us Back to top