EGFR
The epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase of the ErbB family. Four members of the ErbB family have been identified; EGFR (ErbB1, HER1), ErbB2 (HER2), ErbB3 (HER3) and ErbB4 (HER4). EGFR signaling drives many cellular responses.
EGFR Inhibitors |
|
|---|---|
| Cat. No. | Product Name / Activity |
| 5318 | AEE 788 |
| Potent EGFR and VEGFR inhibitor | |
| 6812 | Afatinib dimaleate |
| Potent dual specificity EGFR/HER2 inhibitor; active in vivo | |
| 1276 | AG 1478 hydrochloride |
| Highly potent EGFR-kinase inhibitor | |
| 0414 | AG 490 |
| EGFR-kinase inhibitor. Also JAK2, JAK3 inhibitor | |
| 1555 | AG 825 |
| Selective ErbB2 inhibitor | |
| 5916 | Canertinib dihydrochloride |
| Potent EGFR kinase inhibitor | |
| 6231 | Dacomitinib |
| Potent irreversible pan ErbB inhibitor | |
| 7424 | EMI 48 |
| Inhibitor of EGFR mutants | |
| 7194 | Erlotinib Hydrochloride |
| Potent, reversible EGFR tyrosine kinase inhibitor | |
| 1110 | Genistein |
| EGFR kinase inhibitor. Also estrogen and PPARγ ligand | |
| 2239 | GW 583340 dihydrochloride |
| Potent dual EGFR/ErbB2 inhibitor; orally active | |
| 6813 | Ibrutinib |
| Potent ErbB4 inhibitor; also inhibits BTK | |
| 3000 | Iressa |
| Orally active, selective EGFR inhibitor | |
| 6962 | JBJ-03-142-02 |
| Highly potent EGFR and ErbB2 inhibitor; inhibts wild type and mutated receptors | |
| 3352 | JNJ 28871063 hydrochloride |
| Potent ErbB receptor family inhibitor | |
| 6811 | Lapatinib |
| Potent and selective dual ErbB2 (HER-2) and EGFR inhibitor | |
| 7371 | Neratinib |
| Potent HER2 receptor tyrosine kinase and EGFR kinase inhibitor | |
| 2615 | PD 158780 |
| Potent ErbB receptor family inhibitor | |
| 6349 | Pelitinib |
| Potent and irreversible EGFR inhibitor; orally bioavailable | |
| 4941 | PKI 166 hydrochloride |
| Potent EGFR-kinase inhibitor | |
| 2794 | PP 3 |
| EGFR-kinase inhibitor. Also Src kinase negative control | |
| 3599 | TAK 165 |
| Potent and selective ErbB2 inhibitor | |
| 7640 | Tucatinib |
| Potent and selective ErbB2 inhibitor | |
| 6290 | WZ 4002 |
| Potent mutant-selective EGFR inhibitor | |
Degraders |
|
| Cat. No. | Product Name / Activity |
| 7258 | Gefitinib-based PROTAC® 3 |
| Potent EGFR Degrader | |
| 7886 | HER2 PROTAC® CH7C4 |
| Potent and selective HER2 targeting PROTAC | |
| 7395 | MS 154 |
| Potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant EGFR | |
| 7397 | MS 39 |
| Potent and selective VHL-recruiting Degrader (PROTAC®) of mutant EGFR | |
| 7261 | SJF 1521 |
| Selective EGFR Degrader | |
| 7262 | SJF 1528 |
| Potent EGFR Degrader; also degrades HER2 | |
Controls |
|
| Cat. No. | Product Name / Activity |
| 7396 | MS 154N |
| Negative control for MS 154 (Cat No. 7395) | |
| 7398 | MS 39N |
| Negative control for MS 39 (Cat. No. 7397) | |
The epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase of the ErbB family. Four members of the ErbB family have been identified: EGFR (ErbB1, HER1), ErbB2 (HER2), ErbB3 (HER3) and ErbB4 (HER4).
EGFR signaling is initiated by ligand binding to the extracellular ligand binding domain. This initiates receptor homo-/heterodimerization and autophosphorylation by the intracellular kinase domain, resulting in receptor activation. Following activation, phosphorylation of cytoplasmic substrates occurs and a signaling cascade is initiated that drives many cellular responses, including changes in gene expression, cytoskeletal rearrangement, decreased apoptosis and increased cell proliferation.
External sources of pharmacological information for EGFR :
Literature for EGFR
Tocris offers the following scientific literature for EGFR to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
EGF Receptor Gene Data
| Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
|---|---|---|---|---|
| EGFR | Human | EGFR | NM_005228 | P00533 |
| Mouse | Egfr | NM_207655 | Q01279 | |
| Rat | Egfr | NM_031507 | Q62954 | |
| ErbB2 | Human | ERBB2 | NM_001005862 | P04626 |
| Mouse | Erbb2 | NM_001003817 | P70424 | |
| Rat | Erbb2 | NM_017003 | P06494 | |
| ErbB3 | Human | ERBB3 | NM_001005915 | P21860 |
| Mouse | Erbb3 | NM_010153 | Q61526 | |
| Rat | Erbb3 | NM_017218 | Q62799 | |
| ErbB4 | Human | ERBB4 | NM_001042599 | Q15303 |
| Mouse | Erbb4 | NM_010154 | Q61527 | |
| Rat | Erbb4 | NM_021687 | Q62956 |
Our Angiogenesis in Cancer poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
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