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 |
---|---|---|---|---|
V12121 | AZD9291DA | 1421372-66-8 | AZD9291-DA (also known asMutated EGFR-IN-1 or Osimertinib analog)is a des acryl analogue of AZD9291, which is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. | |
V69303 | Bafisontamab (EMB-01) | 2437210-79-0 | Bafisontamab (EMB-01) is a bispecific antibody targeting EGFR and cMET with anti-tumor activity. | |
V69380 | Barecetamab (ISU-104) | 2275727-74-5 | Barecetamab (ISU-104) is a human anti-ErbB3 monoclonal antibody (mAb). | |
V69333 | BAY 2476568 | 2311901-93-4 | BAY 2476568 is a highly efficient and selective EGFR inhibitor (antagonist) with IC50 of < 0.2 nM against wild-type EGFR and mutant EGFR. | |
V69378 | BEBT-109 | 2050906-40-4 | BEBT-109 is a potent pan-mutation-selective EGFR inhibitor. | |
V69398 | Becotatug (JMT-101) | 2648260-93-7 | Becotatug (JMT-101) is an IgG1 antibody targeting EGFR and can also be coupled with Afatinib and Osimertinib to form an ADC. | |
V69334 | Befotertinib (D-0316) | 1835667-63-4 | Befotertinib (D-0316) is a third-generation EGFR tyrosine kinase inhibitor. | |
V2934 | BIBX 1382 | 196612-93-8 | Falnidamol (formerly known as BIBX 1382) is a potent and selective inhibitor EGFR inhibitor with IC50 of 3 nM and potential anticancer activities; it displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM). | |
V69363 | BPIQ-I (PD 159121) | 174709-30-9 | BPIQ-I (PD 159121) is a potent ATP-competitive EGFR tyrosine kinase inhibitor (TKI). | |
V69364 | CH7233163 | 2923365-71-1 | CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-Del19/T790M/C797S. | |
V69359 | Coprelotamab (GB-221) | 2348469-84-9 | Coprelotamab (GB-221) is an IgG-κ monoclonal antibody (mAb) targeting EGFR2. | |
V69438 | CP-724714 | 383432-38-0 | CP-724714 is a specific, orally bioactive ErbB2 (HER2) tyrosine kinase inhibitor (antagonist) with IC50 of 10 nM. | |
V28786 | CZC-8004 | 916603-07-1 | CZC-8004 (CZC-00008004) is an aminopyrimidine and a pan-kinase inhibitor. | |
V73134 | D-Pro-Phe-Arg-Chloromethylketone | 88546-74-1 | D-Pro-Phe-Arg-Chloromethylketone is an inhibitor (blocker/antagonist) of coagulation factor XII and plasma kallikrein, and plays important roles in thrombosis and inflammation. | |
V79005 | Dacomitinib-d10 dihydrochloride (PF-00299804-d10 (dihydrochloride); PF-299804-d10 (dihydrochloride)) | Dacomitinib-d10 (di-HCl) is the deuterium labelled form of Dacomitinib di-HCl. | ||
V69401 | DBPR112 | 1226549-49-0 | DBPR112 is an orally bioactive fluoropyrimidine-based EGFR inhibitor (antagonist) with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. | |
V69330 | Depatuxizumab (ABT-806) | 1471999-69-5 | Depatuxizumab is a humanized tumor-specific anti-EGFR monoclonal antibody (mAb) that can penetrate the BBB (blood-brain barrier) (brain-penetrant). | |
V69381 | DHFR-IN-4 | 2820126-49-4 | DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor (antagonist) with IC50 of 123 nM. | |
V69357 | dosimertinib-d3 | 2403760-70-1 | Dosimertinib-d3 is a potent orally bioactive EGFR inhibitor. | |
V77074 | Dosimertinib-d5 mesylate | Dosimertinib-d5 (mesylate) is a potent orally bioactive EGFR inhibitor. |