EGFR: Small Molecules and Peptides
EGFR (epidermal growth factor receptor), also known as HER-1, ErbB1, or ErbB, is a transmembrane receptor tyrosine kinase that binds a subset of the EGF family ligands including EGF, Amphiregulin, TGF-alpha, Betacellulin, Epiregulin, HB-EGF, and Epigen. Ligand binding induces EGFR homodimerization as well as heterdimerization with ErbB2, resulting in kinase activation, tyrosine phosphorylation, and cell signaling. EGFR can also be recruited to form heterodimers with the ligand-activated ErbB3 or ErbB4.
EGFR signaling regulates multiple biological functions including cell proliferation, differentiation, motility, and apoptosis. EGFR is overexpressed in a wide variety of tumors and is the target of several anti-cancer drugs. Soluble receptors consisting of the extracellular ligand binding domain are generated by alternate splicing in human and mouse.
Products:
23 results for "EGFR Small Molecules and Peptides" in Products
23 results for "EGFR Small Molecules and Peptides" in Products
EGFR: Small Molecules and Peptides
EGFR (epidermal growth factor receptor), also known as HER-1, ErbB1, or ErbB, is a transmembrane receptor tyrosine kinase that binds a subset of the EGF family ligands including EGF, Amphiregulin, TGF-alpha, Betacellulin, Epiregulin, HB-EGF, and Epigen. Ligand binding induces EGFR homodimerization as well as heterdimerization with ErbB2, resulting in kinase activation, tyrosine phosphorylation, and cell signaling. EGFR can also be recruited to form heterodimers with the ligand-activated ErbB3 or ErbB4.
EGFR signaling regulates multiple biological functions including cell proliferation, differentiation, motility, and apoptosis. EGFR is overexpressed in a wide variety of tumors and is the target of several anti-cancer drugs. Soluble receptors consisting of the extracellular ligand binding domain are generated by alternate splicing in human and mouse.
Products:
Orally active, selective EGFR inhibitor
| Alternate Names: | Gefitinib,ZD 1839 |
| Chemical Name: | N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine |
| Purity: | ≥98% (HPLC) |
EGFR-kinase inhibitor. Also JAK2, JAK3 inhibitor
| Alternate Names: | Tyrphostin AG 490 |
| Chemical Name: | (E)-2-Cyano-3-(3,4-dihydrophenyl)-N-(phenylmethyl)-2-propenamide |
| Purity: | ≥98% (HPLC) |
Highly potent EGFR-kinase inhibitor
| Alternate Names: | Tyrphostin AG 1478 |
| Chemical Name: | N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinanine hydrochloride |
| Purity: | ≥98% (HPLC) |
Potent mutant-selective EGFR inhibitor
| Chemical Name: | N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide |
| Purity: | ≥98% (HPLC) |
Potent dual specificity EGFR/HER2 inhibitor; active in vivo
| Alternate Names: | BIBW2992 |
| Chemical Name: | (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide dimaleate |
| Purity: | ≥98% (HPLC) |
Potent, reversible EGFR tyrosine kinase inhibitor
| Chemical Name: | N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride |
| Purity: | ≥98% (HPLC) |
Potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant EGFR
| Chemical Name: | 3-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-N-(8-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)octyl)propanamide |
| Purity: | ≥98% (HPLC) |
EGFR kinase inhibitor. Also estrogen and PPARγ ligand
| Chemical Name: | 5,7-Dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one |
| Purity: | ≥98% (HPLC) |
Potent and selective dual ErbB2 (HER-2) and EGFR inhibitor
| Chemical Name: | N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine |
| Purity: | ≥98% (HPLC) |
Potent irreversible pan ErbB inhibitor
| Alternate Names: | PF00299804 |
| Chemical Name: | (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide |
| Purity: | ≥98% (HPLC) |
Potent EGFR PROTAC® Degrader; also degrades HER2
| Chemical Name: | (2S,4R)-1-((S)-2-(2-(2-(2-(4-(4-((3-Chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6- yl)phenoxy)ethoxy)ethoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
Highly potent EGFR and ErbB2 inhibitor; inhibts wild type and mutated receptors
| Chemical Name: | (4-Fluorophenyl)methyl N-[2-[(1-methyl-1H-pyrazol-4-yl)amino]-4-pyrimidinyl]-N-[3-[(1-oxo-2-propen-1-yl)amino]phenyl]carbamate |
| Purity: | ≥98% (HPLC) |
Potent HER2 receptor tyrosine kinase and EGFR kinase inhibitor
| Chemical Name: | (2E)-N-[4-[[3-Chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide |
| Purity: | ≥98% (HPLC) |
Potent EGFR kinase inhibitor
| Alternate Names: | CI 1033,PD 183805 |
| Chemical Name: | N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide dihydrochloride |
| Purity: | ≥98% (HPLC) |
Potent EGFR and VEGFR inhibitor
| Chemical Name: | 6-[4-[(4-Ethyl-1-piperazinyl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine |
| Purity: | ≥98% (HPLC) |
Potent dual EGFR/ErbB2 inhibitor; orally active
| Chemical Name: | N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[2-[[[2-(methylsulfonyl)ethyl]amino]methyl]-4-thiazolyl]-4-quinazolinamine dihydrochloride |
| Purity: | ≥97% (HPLC) |
Potent EGFR PROTAC® Degrader
| Alternate Names: | Iressa-based PROTAC 3 |
| Chemical Name: | (2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
Potent and selective VHL-recruiting Degrader (PROTAC®) of mutant EGFR
| Chemical Name: | (2S,4R)-1-((S)-2-(11-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-11-oxoundecanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
Selective EGFR PROTAC® Degrader
| Chemical Name: | (2S,4R)-1-((S)-2-(tert-Butyl)-14-(4-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)phenoxy)-4-oxo-6,9,12-trioxa-3-azatetradecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
Potent ErbB receptor family inhibitor
| Chemical Name: | N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine |
| Purity: | ≥98% (HPLC) |
Potent ErbB receptor family inhibitor
| Chemical Name: | 5E-4-Amino-6-(4-benzyloxy-3-chlorophenylamino)pyrimidine-5-carboxaldehyde N-(2-morpholin-4-ylethyl) oxime hydrochloride |
| Purity: | ≥97% (HPLC) |
Negative control for MS 154 (Cat No. 7395)
| Chemical Name: | 3-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-N-(8-((2-(1-methyl-2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)octyl)propanamide |
| Purity: | ≥98% (HPLC) |
Negative control for MS 39 (Cat. No. 7397)
| Chemical Name: | (2R,4S)-1-((S)-2-(11-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-11-oxoundecanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
