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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V69382 | PROTAC EGFR degrader 8 | 2925923-46-0 | PROTAC EGFR degrader 8 (T-184) is a PROTAC EGFR degrader. |
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V13441 | Pyrotinib (SHR1258) | 1269662-73-8 | Pyrotinib (SHR-1258) is a selective and orally bioavailable, dual kinase inhibitor of EGFR/HER2 [(epidermal growth factor receptor, or HER-1) and the human epidermal growth factor receptor 2 (ErbB2 or HER-2)] with IC50s of 13 and 38 nM, respectively. |
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V69400 | Rezivertinib (BPI-7711) | 1835667-12-3 | Rezivertinib (BPI-7711) is an orally bioactive, selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). |
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V32832 | Rociletinib hydrobromide (CO1686; AVL301) | 1446700-26-0 | Rociletinib hydrobromide (CO-1686; AVL-301; CNX-419), the hydrobromide salt ofRociletinib, is an oral, irreversible/covalent, and mutant-selective EGFR inhibitor (EGFR-TKI) with antitumor activity. |
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V69360 | Serclutamab (PR-1594407; DC-1630423) | 2140172-41-2 | Serclutamab is a humanized chimeric antibody targeting EGFR IgG1-κ. |
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V69434 | Simotinib hydrochloride | 1538617-88-7 | Simotinib HCl is a selective, specific, orally bioavailable EGFR tyrosine kinase inhibitor (TKI) (antagonist) with IC50 of 19.9 nM. |
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V69376 | SIQ17 | 2151881-74-0 | SIQ17 is an EGFR inhibitor that can suppress the activity of EGFR by occupying its ATP binding site, with IC50 of 0.62 nM. |
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V81452 | STX-721 | STX-721 is a mutation-selective inhibitor of EGFR and HER2 exon 20 insertion (ex20ins) mutants. | |
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V69335 | Tephrosin (Deguelinol I; Hydroxydeguelin) | 76-80-2 | Tephrosin is a natural carotenoid with strong anti-tumor activity. |
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V69355 | Theliatinib tartrate (Xiliertinib tartrate; HMPL-309 tartrate) | 2413487-72-4 | Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally bioactive and selective EGFR inhibitor (antagonist) with a Ki of 0.05 nM and IC50 of 3 nM. |
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V69385 | Timigutuzumab (GEXMab73; GT-MAb7.3-GEX; TrastuzuMab-GEX) | 1665274-14-5 | Timigutuzumab (GEXMab73) is a humanized monoclonal antibody (mAb) targeting ErbB2. |
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V31400 | TQB-3804 (EGFR-IN-7) | 2267329-76-8 | TQB-3804 (TQB3804;EGFR-IN-7; compound 34) is a 4th-generation, oralli bioactive and selective EGFR kinase inhibitor (EGFR-TKI, developed in China and disclosed in patent WO2019015655A1) with potential anticancer activity. |
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V69336 | Tucatinib hemiethanolate (Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate) | 1429755-56-5 | Tucatinib (Irbinitinib) hemiethanolate is a potent, orally bioactive, selective HER2 inhibitor (antagonist) with IC50 of 8 nM. |
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V69354 | YK-029A | 2064269-82-3 | YK-029A is an orally bioactive mutant EGFR inhibitor that targets T790M mutation (EGFRT790M) and EGFR exon 20 insertion mutation (EGFRex20ins). |
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V69399 | YS-363 | 2470908-90-6 | YS-363 is a specific and orally bioactive EGFR inhibitor (antagonist) with IC50s of 0.96 nM and 0.67 nM against the wild-type and L858R mutant forms, respectively. |
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V69341 | Zalutumumab | 667901-13-5 | Zalutumumab is a high-affinity, pure human IgG1 monoclonal antibody (mAb) targeting EGFR. |
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V69439 | Zanidatamab (ZW 25) | 2169946-15-8 | Zanidatamab (ZW25) is a human bispecific monoclonal antibody (mAb) targeting 2 different HER2 epitopes (ECD2 and ECD4). |
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V69337 | Zenocutuzumab (MCLA-128; PB4188; R040517) | 1969309-56-5 | Zenocutuzumab (MCLA-128) is a bispecific humanized IgG1 antibody containing two different Fab arms targeting the extracellular domains of HER2 and HER3. |
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V5049 | Zipalertinib (TAS-6417) | 1661854-97-2 | Zipalertinib (TAS6417; CLN-081;TAS-6417) is a novel, potent,orally bioavailableand selective covalent/irreversible EGFR inhibitor with anticancer activity. |
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