EGFR
The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein that constitutes one of four members of the erbB family of tyrosine kinase receptors. The ErbB receptor tyrosine kinase family (RTK class I) consists of ErbB1/EGFR/HER1, and ErbB2-4/HER2-4[1]. Binding of EGFR to its cognate ligands leads to autophosphorylation of receptor tyrosine kinase and subsequent activation of signal transduction pathways that are involved in regulating cellular proliferation, differentiation, and survival. Interestingly, ERbB receptor tyrosine kinases have important roles in human cancer. The gene symbol, ErbB, is derived from the name of a viral oncogene to which these receptors are homologous: Erythroblastic Leukemia Viral Oncogene. Insufficient ErbB signaling in humans is associated with the development of neurodegenerative diseases, such as multiple sclerosis and Alzheimer's disease.[2] Additionally, research revealed that the expression or activation of epidermal growth factor receptor and ErbB2 are altered in many epithelial tumors, and clinical studies indicate that they have important roles in tumor aetiology and progression[3].
[1] Regulation of ERBB Receptors.C.S. Gerbin.Nature Education 2010, 3(9), 36.
[2] The EGF receptor family: spearheading a merger of signaling and therapeutics. E.M. Bublil, Y. Yarden. Curr. Opin. Cell Biol. 2007, 19 (2), 124–134.
[3] ERBB receptors and cancer: the complexity of targeted inhibitors. N.E.Hynes,H.A. Lane. Nat Rev Cancer. 2005, 5(5),341.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 3040 | Abivertinib | Potent oral, irreversible, third-generation EGFR TKI with selectivity for mutant EGFRs | €95.00 | |
| 1653 | AEE 788 | EGFR, ErbB2 and VEGFR tyrosine kinase inhibitor | €80.00 | |
| 1986 | AST 1306 tosylate | ErbB2 and EGFR inhibitor | €90.00 | |
| 4074 | AZ5104 | EGFR inhibitor | Inquire | |
| 2563 | AZD3759 | Potent, orally active, brain-penetrant, EGFR tyrosine kinase inhibitor | €85.00 | |
| 2342 | AZD9291 | Potent oral, irreversible, third-generation EGFR TKI with selectivity for mutant EGFRs | €95.00 | |
| 3862 | BGB-283 | Orally available dual RAF kinase/EGFR inhibitor | Inquire | |
| 1544 | BIBW 2992 | EGFR and ErbB-2/HER2 tyrosine kinase inhibitor | €50.00 | |
| 3853 | BMS-599626 | Potent and selective EGFR and ErbB2 inhibitor | Inquire | |
| 1433 | CI 1033 | EGFR tyrosine kinase inhibitor | €60.00 | |
| 3235 | Dacomitinib | Potent irreversible pan-HER inhibitor | €60.00 | |
| 2680 | EAI045 | Allosteric EGFR inhibitor (L858R/T790M-specific) | €105.00 | |
| 1760 | EGFR Inhibitor [879127-07-8] | Highly selective EGFR tyrosine kinase inhibitor | €120.00 | |
| 3192 | EMI48 | Inhibitor of EGFR triple mutants | €120.00 | |
| 1128 | Erlotinib hydrochloride | EGFR tyrosine kinase inhibitor | €70.00 | |
| 1393 | Gefitinib | EGFR tyrosine kinase inhibitor | €70.00 | |
| 1395 | Lapatinib ditosylate | EGFR and ErbB-2/HER2 tyrosine kinase inhibitor | €80.00 | |
| 1526 | Neratinib | EGFR and ErbB-2/HER2 tyrosine kinase inhibitor | €80.00 | |
| 2955 | NSC 228155 | EGFR tyrosine kinase activator; Inhibitor of KIX-KID interaction | €75.00 | |
| 4144 | Olmutinib | Orally bioavailable and irreversible Tyrosine Kinase Inhibitor | Recently added | Inquire |
| 1632 | OSI 420 | EGFR tyrosine kinase inhibitor | €90.00 | |
| 1665 | Pelitinib | EGFR tyrosine kinase inhibitor | €90.00 | |
| 2920 | Poziotinib | Irreversible pan-HER inhibitor | €95.00 | |
| 3232 | TAK-788 | Potent and selective EGFR and ErbB-2/HER2 tyrosine kinase inhibitor | €70.00 | |
| 3802 | TAS6417 | EGFR inhibitor | Inquire | |
| 1411 | Vandetanib | VEGFR and EGFR tyrosine kinase inhibitor | €50.00 | |
| 1506 | WZ 4002 | EGFR kinase inhibitor (T790M specific) | €70.00 | |