The epidermal growth factor receptor (EGFR; ErbB1) is a member of the epidermal growth factor RTK (receptor tyrosine kinases) family, which also includes 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-), 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 |
---|---|---|---|---|
V0207 | Chrysophanic Acid (Chrysophanol) | 481-74-3 | Chrysophanic acid (also called Chrysophanol), a naturally occuring anthraquinone isolated from Dianella longifolia, is a selective and potent inhibitor of EGFR/mTOR (epidermal growth factor (EGF) receptor/mammalian target of rapamycin) with potential anti-obesity and antitumor activity. | |
V0543 | CL-387785 (EKI-785) | 194423-06-8 | CL-387785 (CL387785; WAY-EKI 785; EKI 785; EKI785) is a novel, potent, covalent / irreversible, and selective EGFR inhibitor with potential anticancer activity. | |
V0548 | CNX-2006 | 1375465-09-0 | CNX-2006 (CNX2006), a CO-1686 analog, is a covalent / irreversible and mutant-selective EGFR inhibitor with potential antitumor activity. | |
V0557 | CP-724714 | 537705-08-1 | CP-724714 (CP724714) is an orally bioavailable,potent, selective inhibitor of HER2/ErbB2 with potential anticancer activity. | |
V0558 | Dacomitinib (PF-299804, PF-299) | 1110813-31-4 | Dacomitinib (formerly aslo known as PF299804, PF299; trade name:Vizimpro) is an orally bioavailable, highly selective, irreversible/covalent, 2nd generation pan-ErbB inhibitor, mostly to EGFR, with IC50 values of 6 nM, 45.7 nM and 73.7 nM for inhibiting EGFR,ERBB2, andERBB4, respectively in cell-free assays. | |
V19109 | Dacomitinib hydrate (PF-00299804; PF-299804) | 1042385-75-0 | escription: Dacomitinib (aslo known as PF299804, PF299; trade name: Vizimpro) is a novel, potent, orally bioavailable, highly selective, irreversible, second generation pan-ErbB inhibitor, mostly to EGFR with with IC50 of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively in cell-free assays. | |
V4000 | EBE-A22 | 229476-53-3 | EBE-A22 is aN-methyl derivative of PD-153035 which exhibits a very high affinity and selectivity for the epidermal growth factor receptor tyrosine kinase (EGF-R TK) and shows a remarkable cytotoxicity against several types of tumor cell lines. | |
V0544 | Erlotinib (OSI744, Tarceva) | 183321-74-6 | Erlotinib (formerly OSI744, trade name:Tarceva) isa quinazoline-based EGFR (epidermal growth factor receptor) inhibitor with potential antineoplastic activity. | |
V0533 | Erlotinib HCl (OSI-744, Tarceva) | 183319-69-9 | Erlotinib HCl (formerly OSI-744, OSI744; trade name:Tarceva), the hydrochloride salt of erlotinib, is an EGFR (epidermal growth factor receptor) inhibitor with antitumor activity. | |
V0534 | Gefitinib (ZD 1839) | 184475-35-2 | Gefitinib (formerly ZD1839, ZD-1839 or trade name: Iressa) is a potent and orally bioavailable EGFR inhibitor with potential anticancer activity. | |
V0571 | Genistein (NPI031L; BIO-00; G2535; PTI G-4660; SIPI9764I) | 446-72-0 | Genistein (NPI-031L;BIO-300; G-2535; PTI-G-4660; SIPI-9764I), a naturally occuring isoflavonoid isolated from soy products, is a potent multi-kinase inhibitor with potential anticancer activity against various cancers. | |
V0569 | Icotinib (BPI2009) | 610798-31-7 | Icotinib (formerly known as BPI-2009; trade name Conmana), a side chain-cyclized form of erlotinib, is an orally available and specific EGFR inhibitor with potent anticancer activity. | |
V3302 | Icotinib Hydrochloride (BPI-2009) | 1204313-51-8 | Icotinib HCl (formerly known as BPI-2009 HCl), the hydrochloride salt ofIcotinib and an macrocyclic analog of erlotinib, is an orally bioavailable, potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R). | |
V40813 | JBJ-04-125-02 HCL | 2140807-05-0 | JBJ-04-125-02 HCL is a novel, highly potent, mutant-specific, allosteric and orally bioavailable EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. | |
V0540 | Lapatinib (GW-572016, Tykerb, Tyverb) | 231277-92-2 | Lapatinib (formerly GW572016, trade namesTykerb&Tyverb), usually used in the Ditosylate form, is a potent, orally bioavailable dual EGFR/ErbB2 inhibitor with potential anticancer activity. | |
V0535 | Lapatinib Ditosylate (GW-572016, Tykerb) | 388082-77-7 | Lapatinib Ditosylate (formerly GW-572016, GW572016; trade names Tykerb and Tyverb) is an orally bioavailable medication acting as an EGFR (epidermal growth factor receptor) and ErbB2 inhibitor with antineoplastic activity. | |
V3697 | Lazertinib (YH25448,GNS-1480) | 1903008-80-9 | Lazertinib (formerly known as GNS-1480; YH-25448; GNS1480; YH25448;LECLAZA) is an oral, highly mutant-selective and irreversible 3rd generation EGFR TKI (Tyrosine-kinase inhibitors) approved in 2021 for the treatment of lung cancer (NSCLC). | |
V3179 | Lifirafenib (BGB-283) | 1446090-79-4 | Lifirafenib (formerly BGB-283, Beigene-283) is a potent inhibitor of theRAF kinasesandEGFRin biochemical assays withIC50values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant respectively. | |
V37850 | Mobocertinib (TAK788, AP32788) | 1847461-43-1 | Mobocertinib (TAK-788; AP-32788; Exkivity), a drug used for the treatment of non-small cell lung cancer (NSCLC), is a novel, highly potent, irreversible and orally bioavailable inhibitor of EGFR and HER2 oncogenic mutants (e.g. exon 20 insertions), and exhibits high selectivity over WT EGFR. | |
V11726 | Naquotinib free base | 1448232-80-1 | Naquotinib (ASP 8273; ASP-8273; ASP8273) is an irreversible/covalent and 3rd-generation inhibitor of epidermal growth factor receptor (EGFR) with potential antitumor activity. |