EGFR
Epidermal growth factor receptor; ErbB-1; HER1
The EGFR family of receptor tyrosine kinases (RTK) comprises four distinct receptors: the EGFR (also known as ErbB-1/HER1), ErbB-2 (neu, HER2), ErbB-3 (HER3) and ErbB-4 (HER4). All EGFR family members are characterized by a modular structure consisting of an extracellular ligand-binding domain, a single hydrophobic transmembrane region, and the intracellular part harbouring the highly conserved tyrosine kinase domain. The ErbB family of receptor tyrosine kinases (RTKs) couples binding of extracellular growth factor ligands to intracellular signaling pathways regulating diverse biologic responses, including proliferation, differentiation, cell motility, and survival. Ten growth factors and their ErbB specificities are: EGF, amphiregulin (AR), and TGF bind ErbB-1; betacellulin, and epiregulin bind both ErbB-1 and ErbB-4; the neuregulins (also called heregulins and Neu differentiation factors) NRG-1 and NRG-2 bind ErbB-3 and ErbB-4; and NRG-3 and NRG-4 bind ErbB-4. No known ligand binds ErbB-2. The three best characterized signaling pathways induced through ErbBs are Ras-mitogen-activated protein kinase (Ras-MAPK), phosphatidylinositol 3 kinase-protein kinase B (PI3K-PKB/Akt), and phospholipase C-protein kinase C (PLC-PKC) pathways.
EGFR Isoform Specific Products
All Product Categories
-
EGFR Inhibitors
(1042)
View all products
-
EGFR Agonists
(4)
View all products
-
EGFR Antagonists
(5)
View all products
-
EGFR Activators
(8)
View all products
-
EGFR Modulators
(7)
View all products
-
EGFR Chemicals
(3)
View all products
-
EGFR Inducers
(4)
View all products
-
EGFR Degraders
(45)
View all products
-
EGFR Controls
(6)
View all products
-
EGFR Substrate
(1)
View all products
-
EGFR Ligands
(19)
View all products
-
ErbB2/HER2 Proteins
(40)
View all products
-
ErbB3/HER3 Proteins
(15)
View all products
-
EGFR Proteins
(47)
View all products
-
ErbB4/HER4 Proteins
(10)
View all products
-
EGFR Related Products (1265)
Related Products (1265)
-
Recombinant Proteins (112)
-
Antibodies (19)
-
EGFR Isoform Comparison
-
EGFR-IN-121
0 ImagesCat. No.: HY-162788CAS No.: 418799-16-3EGFR-IN-121 (compound 15) is a EGFR and VEGFR-2 dual inhibitor with IC50s of 84 and 3.5 nM, respectively.
-
NODAGA-NHS
0 ImagesCat. No.: HY-156991CAS No.: 1407166-70-4Synonyms: NODA-GA-NHS esterNODAGA-NHS (NODA-GA-NHS ester) is the activated ester form of the NODAGA chelator. NODAGA-NHS conjugates with Trastuzumab (HY-P9907) to form NODAGA-Trastuzumab, a conjugate that can chelate 64Cu for the preparation of radiotracers. NODAGA-NHS covalently binds to the amino group of lactosamine derivatives to form radiotracer precursors. [64Cu]NODAGA-trastuzumab enables PET imaging of tumors expressing HER2. NODAGA-NHS is used in studies of HER2-positive breast cancer and ovarian adenocarcinoma.
-
PKI-166 hydrochloride
0 ImagesCat. No.: HY-110328CAS No.: 2230253-82-2PKI-166 hydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.
-
ZSH-2117
0 ImagesCat. No.: HY-174415ZSH-2117 is an NEDD4-recruiting EGFR PROTAC degrader. ZSH-2117 shows an IC50 of 13 nM against EGFRL858R/T790M/C797S, induces EGFR proteasome-dependent degradation, inhibits the downstream signaling pathways of EGFR, including the phosphorylation of AKT and ERK, suppresses cancer cell proliferation, and exhibits in vivo anti-tumor activity. ZSH-2117 can be used in research related to non-small cell lung cancer.
-
TX-1123
0 ImagesCat. No.: HY-121828CAS No.: 157397-06-3TX-1123 is a potent protein tyrosine kinase (PTK) inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC. TX-1123 is a cyclo-oxygenase (COX) inhibitor with IC50 values of 1.16 μM and 15.7 μM for COX2 and COX1, respectively. TX-1123 has low mitochondrial toxicity. TX-1123 can be used in research of cancer.
-
Multi-kinase-IN-4
0 ImagesCat. No.: HY-149407Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer.
-
HSP90-IN-11
0 ImagesCat. No.: HY-146325CAS No.: 2986564-20-7HSP90-IN-11 is a HSP90 inhibitor with an IC50 of 27.8 nM. HSP90-IN-11 inhibits the activity of HSP90, which in turn induces rapid degradation of EGFR and Akt proteins in non-small cell lung cancer (NSCLC) cells. HSP90-IN-11 induces accumulation of the G1 subphase cell population in NSCLC cells, activates caspase-3, caspase-8, caspase-9 and PARP, thereby triggering apoptosis. HSP90-IN-11 exhibits antiproliferative activity in colorectal cancer and NSCLC cells. HSP90-IN-11 can be used for the research of colorectal cancer and non-small cell lung cancer.
-
Eps8 peptide 327
0 ImagesCat. No.: HY-P10994CAS No.: 1988684-26-9Synonyms: Eps8(327-335)Eps8 peptide 327 is an HLA-A*2402-restricted peptide antigen derived from Eps8 protein. Eps8 peptide 327 has potent antitumor activity with significant cytotoxicity. Eps8 peptide 327 effectively inhibits cancer cells proliferation, induces apoptosis and disrupts EGFR signal pathway by inhibiting downstream signals (such as IL-2, TNF-α and IFN-γ) expression and the Eps8/EGFR interaction. Eps8 peptide 327 significantly inhibits tumor growth in HT-29 xenograft mcie models.
-
EGFR/HER2-IN-11
0 ImagesCat. No.: HY-160613CAS No.: 1346176-20-2EGFR/HER2-IN-11 (compound 20) is an orally active dual inhibitor for human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC50s of 7.7 and 22 nM, respectively. EGFR/HER2-IN-11 exhibits antitumor efficacy and inhibits proliferation against cancer cells BT-474 with GI50 of 601 nM.
-
WGYRGFYC
0 ImagesCat. No.: HY-P11590WGYRGFYC (WC8) is a selective HER2-targeting peptide that binds specifically to HER2 by mimicking the antigen-binding site of trastuzumab. The DOTA precursor of WGYRGFYC has a KD of 61.20 nM for HER2. WGYRGFYC enables specific and highly sensitive detection of HER2 expression in HER2-positive breast cancer cells and tumor tissues, and monitors the dynamic downregulation of HER2 expression. WGYRGFYC rapidly distributes to target tissues and is efficiently cleared from non-target tissues via the kidneys, generating an ideal tumor-to-background ratio in imaging; it is a component of the PET radiotracer Ga-DOTA-WC8. WGYRGFYC exhibits no significant cytotoxicity in breast cancer cells, and can be used for non-invasive imaging diagnosis and therapeutic efficacy evaluation of HER2-positive breast cancer.
-
EGFR-IN-154
0 ImagesCat. No.: HY-173188EGFR-IN-154 (compound 4c) is an EGFR inhibitor with EC50 values of 0.16 μM, 21.73 μM and 41.56 μM against EGFR Del19, EGFR WT and EGFR L858R, respectively. EGFR-IN-154 shows anticancer activity on various cance cell lines. EGFR-IN-154 induces mitochondrial apoptosis, and decreases pERK1/2 and pAkt levels, but increases pJNK and pp38 levels.
-
GLUT1/EGFR-IN-1
0 ImagesGLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of GLUT1 and EGFR. GLUT1/EGFR-IN-1 can simultaneously act on the EGFR tyrosine kinase ATP-binding site and inhibit GLUT1-mediated energy metabolism, resulting in reductions in ATP, MMP, intra-cellular lactic acid, and EGFR nuclear transfer. GLUT1/EGFR-IN-1 can be used for nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC) research.
-
CGP-59326
0 ImagesCat. No.: HY-117852CAS No.: 173458-56-5Synonyms: TRX-13
-
EGFR/c-Met-IN-1
0 ImagesCat. No.: HY-163006CAS No.: 3020728-68-8EGFR/c-Met-IN-1 (compound TS-41) is a dual-target inhibitor of EGFR/c-Met. The IC50 for inhibiting EGFRL858R and c-Met is 68.1 nM and 0.26 nM respectively. . EGFR/c-Met-IN-1 induces apoptosis and cell cycle arrest in A549-P cells, downregulating the phosphorylation of EGFR, c-Met, and downstream AKT. EGFR/c-Met-IN-1 inhibits tumor growth in vitro and in vivo.
-
EGFR/VEGFR2-IN-12
0 ImagesCat. No.: HY-182005EGFR/VEGFR2-IN-12 is a dual EGFR/VEGFR2 inhibitor, with an IC50 value of 64 nM against human EGFR and an IC50 value of 74 nM against human VEGFR2. EGFR/VEGFR2-IN-12 inhibits the phosphorylation of EGFR and VEGFR2, induces cell cycle arrest at the G1/S phase, activates apoptotic pathways, promotes PARP-1 cleavage, exhibits low micromolar antiproliferative activity, and shows much higher selectivity for cancer cells than normal cells. EGFR/VEGFR2-IN-12 is applicable for cancer-related research.
-
LY456236 free base
0 ImagesCat. No.: HY-103566ACAS No.: 338738-57-1LY456236 free base is a selective, non-competitive and orally active antagonist of glutamate receptor 1 (mGlu1), which can inhibit phosphatidylinositol hydrolysis with an IC50 of 0.145 μM. LY456236 free base can also inhibit EGFR, with an IC50 of 0.918 μM. LY456236 free base blocks cell proliferation by inhibiting the MAPK pathway, reversing the anti-apoptotic effect of DHPG (HY-12598A). LY456236 free base can be used in epilepsy research.
-
EGFR-IN-194
0 ImagesCat. No.: HY-181166EGFR-IN-194 is a potent EGFR tyrosine kinase inhibitor with an IC50 of 54.3 nM against human EGFR. EGFR-IN-194 induces apoptosis, inhibits migration in cancer cells, selectively promotes invasion in cancer cells, and exhibits antiproliferative effects across multiple cancer cell lines. EGFR-IN-194 can be used for the research of prostate adenocarcinoma, non-small cell lung carcinoma, breast carcinoma, chronic myeloid leukemia.
-
EGFR-IN-71
0 ImagesCat. No.: HY-150781CAS No.: 2676155-98-7EGFR-IN-71 is a potent narrow spectrum epidermal growth factor receptor (EGFR) inhibitor with IC50 values of 3.7 μM. EGFR-IN-71 can be used for researching chordoma. EGFR-IN-71 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
