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EGFR

EGFR

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.

EGFR related products

Structure Cat No. Product Name CAS No. Product Description
(E)-AG 99 (AG99) V33525 (E)-AG 99 (AG99) 122520-85-8 (E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
AC480 (BMS599626) V0554 AC480 (BMS599626) 714971-09-2 AC480 (also known as BMS-599626) is a novel, potent, orally bioavailable, selective and efficacious inhibitor of HER1/2 (human epidermal growth factor receptors) with potential anticancer activity.
AEE788 (NVP-AEE788) V0504 AEE788 (NVP-AEE788) 497839-62-0 AEE788 (NVP-AEE-788; NVP-AEE788) is a novel, potent and orally bioavailable inhibitor of multiple receptor tyrosine kinase such as EGFR (epidermal growth factor receptor) and HER2/ErbB2 with potential antitumor activity.
AG 30 (Tyrphostin AG30) V10440 AG 30 (Tyrphostin AG30) 122520-79-0 An antimicrobial peptide with angiogenic properties, AG-30/5C, activates human mast cells through the MAPK and NF-κB pathways.
AG-1557 V3989 AG-1557 189290-58-2 AG-1557 is a novel and potent inhibitor of epidermal growth factor receptor tyrosine(EGFR)kinase.
AG-18 (RG50858, TX-825) V0549 AG-18 (RG50858, TX-825) 118409-57-7 AG-18 (also known as RG-50810, RG-50858, TX 825, Tyrphostin A23 andTyrphostin AG-18) isa novel and potentEGFRinhibitor with anIC50andKi of 35 and 11 μM, respectively.
AG555 V7601 AG555 133550-34-2 AG 555 (Tyrphostin AG 555) is a potent antiretroviral active molecule and a potent and specific EGFR inhibitor that blocks Cdk2 activation.
AV-412 V30518 AV-412 451492-95-8 AV-412 free base (MP-412 free base) is an EGFR inhibitor.
AZ5104 V0541 AZ5104 1421373-98-9 AZ5104 (AZ-5104), a demethylated and active metabolite of Osimertinib (AZD-9291), isanirreversible EGFRinhibitor with potential antitumor activity.
BMS-690514 V3490 BMS-690514 859853-30-8 BMS-690514 is a novel, potent and orally bioavailable inhibitor of EGFR [human epidermal growth factor receptor (HER) 1] and VEGFR (vascular endothelial growth factor receptors) with IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.
CL-387785 (EKI-785) 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.
CNX-2006 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.
CP-724714 V0557 CP-724714 537705-08-1 CP-724714 (CP724714) is an orally bioavailable,potent, selective inhibitor of HER2/ErbB2 with potential anticancer activity.
EBE-A22 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.
JBJ-04-125-02 V40813 JBJ-04-125-02 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.
Lifirafenib (BGB-283) 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.
O-去甲基埃罗替尼盐酸盐 V0562 OSI-420 (Desmethyl Erlotinib) HCl 183320-51-6 OSI-420 HCl (also known as CP-473420; OSI420; Desmethyl Erlotinib), the demethylated and active metabolite of erlotinib, is a potent, selective, orally bioavailable and ATP competitive inhibitor of tyrosine kinase EGFR with potential antineoplastic activity.
PD153035 HCl (SU5271; ZM252868) V0568 PD153035 HCl (SU5271; ZM252868) 183322-45-4 PD153035 HCl (SU-5271; ZM-252868), the hydrochloride salt of PD153035(also called PD-153035), is an ATP competitive EGFR inhibitor with potential antineoplastic activity.
PD168393 (PD-168393) V0547 PD168393 (PD-168393) 194423-15-9 PD168393 (PD-168393)is covalent / irreversible, cell-permeable and ATP-competitive EGFR inhibitor with potential anticancer activity.
RG 13022 V9597 RG 13022 136831-48-6 RG13022 is a tyrosine kinase inhibitor (TKI); the IC50 for inhibiting EGF receptor autophosphorylation is 4 μM.
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