The epidermal growth factor receptor (EGFR; ErbB1) is a member of the epidermal growth factor RTK (receptor tyrosine kinases) family, along with 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-α), 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 |
|---|---|---|---|---|
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V99924 | Asandeutertinib | 1638281-46-5 | Asandeutertinib (Osimertinib-d3; AZD-9291-d3) is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with antitumor effects. |
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V98031 | BPI-15086 | 1644502-33-9 | BPI-15086 is an oral, potent, irreversible, mutation-selective EGFR and T790M resistance-mutant tyrosine kinase inhibitor. |
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V98985 | CLM3 | 1312024-59-1 | CLM3 is a pyrazolopyrimidine derivative and a multi-tyrosine kinase inhibitor. |
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V99889 | EGFR-IN-121 | 418799-16-3 | EGFR-IN-121 (Compound 15) is a dual inhibitor of EGFR and VEGFR-2 with IC50 of 84 nM and 3.5 nM, respectively. |
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V99937 | EGFR/Akt-IN-1 | EGFR/Akt-IN-1 (Compound 17) is a potent inhibitor of EGFR/Akt with IC50 of 12.89 μM and 10.88 μM in A549 cells, respectively. | |
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V98368 | EGFR/PI3Kα-IN-1 | EGFR/PI3Kα-IN-1 (Compound 30k) is a dual EGFR/PI3Kα inhibitor with IC50 of 3.6 nM (EGFRL858R/T790M) and 30 nM (PI3Kα), respectively. | |
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V98447 | Herceptide | 3027722-28-4 | Herceptide (HER2 targeting peptide) is a HER2 targeting peptide that can be further conjugated with the near-infrared fluorescent dye indocyanine green (ICG) for the development of phototherapeutic drugs. |
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V98053 | Neptinib | 2085843-51-0 | Neptinib (NEP010) is an oral afatinib derivative with stronger antitumor activity than afatinib by improving pharmacokinetics. |
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V99671 | NRC-2694-A | 1172626-99-1 | NRC-2694-A is an oral EGFR tyrosine kinase inhibitor. |
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V98068 | Si306 | 1640012-88-9 | Si306 is a Src inhibitor with antitumor activity. |
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V98980 | SST0116CL1 | 1799802-29-1 | SST0116CL1 is a HSP90 inhibitor (IC50: 0.21 μM). |
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