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 |
---|---|---|---|---|
V0340 | WHI-P154 | 211555-04-3 | WHI-P154 is a novel, potent and selective JAK3 (Janus kinase) inhibitor with potential antitumor activity. | |
V0565 | WZ3146 | 1214265-56-1 | WZ3146 (WZ-3146) is a covalent / irreversible and mutant-selective inhibitor of EGFR (L858R and E746_A750) with potential anticancer activity. | |
V0552 | WZ4002 | 1213269-23-8 | WZ4002 (WZ-4002) is a covalent/irreversible and mutant-selective EGFR (e.g. L858R/T790M) inhibitor with potential antitumor activity. | |
V0566 | WZ8040 | 1214265-57-2 | WZ8040 is a novel, potent, mutant-selective and covalent / irreversible EGFR(T790M) inhibitor with potential anticancer activity, it does not inhibit thephosphorylation of ERBB2 (T798I). | |
V0538 | Zorifertinib (AZD3759; AZD-3759; zorifertinibum) | 1626387-80-1 | Zorifertinib (formerly AZD3759; AZD-3759; zorifertinibum) is a novel, potent, orally bioavailable, CNS (central nervous system)-penetrant EGFR (epidermal growth factor receptor) inhibitor with potential antitumor activity. |