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
(1054)
View all products
-
EGFR Agonists
(4)
View all products
-
EGFR Antagonists
(5)
View all products
-
EGFR Activators
(9)
View all products
-
EGFR Modulators
(7)
View all products
-
EGFR Chemicals
(3)
View all products
-
EGFR Inducers
(5)
View all products
-
EGFR Degraders
(54)
View all products
-
EGFR Controls
(6)
View all products
-
EGFR Substrate
(1)
View all products
-
EGFR Ligands
(20)
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 (1295)
Related Products (1295)
-
Recombinant Proteins (112)
-
Antibodies (19)
-
EGFR Isoform Comparison
-
Multi-target kinase inhibitor 3
0 ImagesCat. No.: HY-169216Multi-target kinase inhibitor 3 (compund 6i) is a multi-kinase target inhibitor with anticancer activity. Multi-target kinase inhibitor 3 inhibits EGFR, HER2, VEGFR-2, and CDK2 with IC50s of 0.063 μM, 0.054 μM, 0.119 μM, and 0.448 μM, respectively. Multi-target kinase inhibitor 3 has a good inhibitory effect on breast cancer cells MCF-7, with an IC50 of 6.10 μM.
-
EGFR-IN-197
0 ImagesCat. No.: HY-181502CAS No.: 3060883-16-8EGFR-IN-197 is an EGFR inhibitor with IC50 values of 19.5 nM and 12.0 nM against EGFRL858R/T790M and EGFRL858R/T790M/C797S, respectively. EGFR-IN-197 arrests the cell cycle of NCI-H1975 cells at the G2/M phase, while inhibiting their proliferation, colony formation and migration; it also inhibits mitochondrial translocation and upregulates mitochondrial H2S levels. EGFR-IN-197 disrupts anti-apoptotic signaling pathways by regulating apoptosis-related proteins; it induces DNA damage and activates pro-apoptotic pathways to trigger apoptosis. EGFR-IN-197 can be used in studies related to non-small cell lung cancer (NSCLC).
-
Autophagy-IN/Ferroptosis inducer-modulator-1
0 ImagesCat. No.: HY-187191Autophagy-IN/Ferroptosis inducer-modulator-1 is a dual-functional molecule that acts as an Autophagy inhibitor and a Ferroptosis inducer. Autophagy-IN/Ferroptosis inducer-modulator-1 downregulates GPX4 expression, elevates ROS levels and reduces mitochondrial membrane potential. Autophagy-IN/Ferroptosis inducer-modulator-1 arrests the cell cycle of non-small cell lung cancer (NSCLC) cells, induces mild apoptosis and inhibits autophagy. Autophagy inhibition induced by Autophagy-IN/Ferroptosis inducer-modulator-1 acts upstream of ferroptosis to produce a synergistic effect. Autophagy-IN/Ferroptosis inducer-modulator-1 exhibits anti-tumor activity against both human tumor cells and zebrafish xenograft models. Autophagy-IN/Ferroptosis inducer-modulator-1 can be used for research related to non-small cell lung cancer.
-
FS102
0 ImagesCat. No.: HY-P991235Synonyms: BMS-986186FS102 is a selective Fc fragment with antigen binding (Fcab) that targets HER2 with a KD value of 0.8 nM. FS102 induces the degradation of HER2, activates Caspase 3/7 and disrupts the integrity of the cell membrane, triggering apoptosis of tumor cells. FS102 is promising for research of cancers such as breast cancer, gastric cancer, and colorectal cancer.
-
Dyrk1A-IN-15
0 ImagesCat. No.: HY-179599CAS No.: 1448757-02-5Dyrk1A-IN-15 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 19 nM. Dyrk1A-IN-15 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-15 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-15 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-15 has potential for glioblastoma (GBM) research.
-
NS-062
0 ImagesCat. No.: HY-123891CAS No.: 2226257-92-5NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC50 of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model.
-
PRMT5/EGFR-IN-1
0 ImagesCat. No.: HY-163434CAS No.: 3034402-59-7PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors.
-
EGFR/c-SRC-IN-1
0 ImagesCat. No.: HY-184274EGFR/c-SRC-IN-1 is a blood-brain barrier-impermeable, ATP-competitive dual-target inhibitor of EGFR/c-SRC, with an IC50 of 0.05 μM against EGFR and an IC50 of 0.07 μM against c-SRC. EGFR/c-SRC-IN-1 shows selectivity toward ABL-2 and VEGFR-2 kinases. EGFR/c-SRC-IN-1 triggers endogenous apoptosis by upregulating p53 and Bax, downregulating Bcl-2, and altering the Bax/Bcl-2 ratio. EGFR/c-SRC-IN-1 can be used in the research of non-small cell lung cancer, hepatocellular carcinoma, and triple-negative breast cancer.
-
EGFR WT/T790M-IN-3
0 ImagesCat. No.: HY-175292EGFR WT/T790M-IN-3 is an irreversible covalent EGFRWT and EGFRT790M inhibitor with IC50s value of 28.1 and 24.6 nM. EGFR WT/T790M-IN-3 hampers tubulin polymerization through IC50 value of 5.1 μM. EGFR WT/T790M-IN-3 shows significant anti-proliferative effects on HCT116 and T47D cells, with IC50 values of 3.12 and 4.12 μM, respectively. EGFR WT/T790M-IN-3 can be used for the study of cancers such as non-small cell lung cancer, colon cancer and breast cancer.
-
EGFR/HDAC-IN-1
0 ImagesCat. No.: HY-173520EGFR/HDAC-IN-1 (Compound 22c2) is a potent dual inhibitor of epidermal growth factor receptor (EGFR) and histone deacetylase (HDAC) with IC50 values of 4.81 nM, 119.4 nM and 354.8 nM for EGFR, HDAC1 and HDAC3, respectively. EGFR/HDAC-IN-1 blocks the EGFR signaling pathway and affects the histone acetylation status, thereby inhibiting tumor cell proliferation. EGFR/HDAC-IN-1 is promising for research of non-small cell lung cancer (NSCLC).
-
EGFR T790M/L858R-IN-2
0 ImagesEGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity.
-
Lapatinib-13C215N
0 ImagesCat. No.: HY-W777297CAS No.: 1246819-08-8Lapatinib-13C2,15N Ditosylate is the 13C- and 15N-labeled Lapatinib ditosylate (HY-50898A). Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
-
EGFR-IN-151
0 ImagesCat. No.: HY-173038EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. EGFR-IN-151 inhibits the proliferation of a variety lung cancer cells (IC50s for NCI-H1781, HCC827, NCI-H3255 and NCI-H1975 is 11.7, 5.19, 7.32 and 1.53 μM, respectively), inhibits the colony formation and migration of H1975, arrests the cell cycle at G1 phase, and induces apoptosis in H1975.
-
EGFR-IN-118
0 ImagesCat. No.: HY-161866EGFR-IN-118 (Compound 4a) is an inhibitor for the tyrosine kinase EGFR. EGFR-IN-118 demonstrates anti-cancer property, inhibiting the proliferation of MCF-7 and PC3 with IC50 of 2.53 and 3.25 µg/ml. EGFR-IN-118 exhibits antioxidant efficacy, inhibiting the DPPH free radicals with IC50 of 10.04 µg/ml.
-
EGFR kinase-IN-8
0 ImagesCat. No.: HY-180922CAS No.: 3081622-35-4EGFR kinase-IN-8 (Compound H8b) is an EGFR inhibitor. EGFR kinase-IN-8 potently inhibits both triple-mutated EGFRL858R/T790M/C797S (IC50 = 3.86 nM) and double-mutated EGFRL858R/T790M (IC50 = 1.23 nM). EGFR kinase-IN-8 suppresses EGFR phosphorylation and downstream AKT, STAT3, and MAPK signaling. EGFR kinase-IN-8 exhibits anticancer activity against non-small cell lung cancer.
