The receptor tyrosine kinase family of the epidermal growth factor, which also includes HER2/neu (ErbB2), ErbB3 (HER3), and ErbB4 (HER4), includes the epidermal growth factor receptor (EGFR; ErbB1). 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 |
|---|---|---|---|---|
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V69379 | (3S,4S)-PF-06459988 | 1858291-14-1 | (3S, 4S)-PF-06459988 is the less active S-enantiomer of PF-06459988. |
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V33525 | (E)-AG 99 (AG99) | 122520-85-8 | (E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor. |
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V51518 | (E/Z)-AG490 | 134036-52-5 | (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is the racemate of (E)-AG490 and (Z)-AG490. |
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V87036 | (Rac)-JBJ-04-125-02 acetate | (Rac)-JBJ-04-125-02 acetate is the racemate of JBJ-04-125-02, a potent, mutant-selective, allosteric and orally active EGFR inhibitor. | |
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V88019 | (Z)-RG-13022 | 149286-90-8 | (Z)-RG-13022 is a tyrosine kinase (TK) inhibitor that preferentially inhibits EGFR TK activity and inhibits EGF-stimulated cultured cell growth. |
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V83079 | (±)-Norcantharidin | 29745-04-8 | (±)-Norcantharidin (Endothall anhydride) is a synthetic anticancer agent that functions as a dual inhibitor of EGFR and c-Met in human colon cancers. |
![1-Methyl-1H-pyrrolo[2,3-b]pyridine](http://www.invivochem.com/upload/1124/V123606.png)
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V123606 | 1-Methyl-1H-pyrrolo[2,3-b]pyridine | 27257-15-4 | 1-Methyl-1H-pyrrolo[2,3-b]pyridine is a 7-azaindole derivative that can bind to the EGFR kinase domain. |
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V92474 | 13(S)-HPODE | 33964-75-9 | 13(S)-HPODE is a linoleic acid metabolite found in some plants and mammals. |
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V69423 | 2′-Thioadenosine (PD157432) | 136904-69-3 | 2'-Thioadenosine (PD157432) is a selective and irreversible inhibitor of ErbB-1 and ErbB-2 with IC50 of 45 µM for ErbB-2. |
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V77564 | 2-2(t)aptamer sodium | 2-2(t) aptamer sodium is a trimeric complex of nucleic acid aptamer (2-2), containing 42 nucleotides, targeting ErbB-2. | |
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V102893 | 4-Epidoxycycline | 6543-77-7 | 4-Epidoxycycline is a hepatic metabolite of the antibiotic doxycycline and has no antibiotic activity in mice. |
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V101861 | 4-Methyl erlotinib | 1346601-52-2 | 4-Methylerlotinib is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. |
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V97045 | 4-Methyl erlotinib (Standard) | 1346601-52-2 | 4-Methyl Erlotinib (Standard) is the analytical standard for 4-methyl Erlotinib. |
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V2347 | 4557W | 179248-61-4 | 4557Wis a potent and reversible inhibitor of EGFR(Epidermal growth factor receptor) and c-ErbB2 (IC50s = 20 and 79 nM, respectively). |
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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. |
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V3500 | AC480 HCl | 873837-23-1 | AC480 HCl (also known as BMS-599626 HCl) is a novel, potent, orally bioavailable, selective and efficacious inhibitor of HER1 and HER2 (human epidermal growth factor receptors) with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. |
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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. |
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V114168 | AfaPhos1 | AfaPhos1 is a novel EGFR phosphorylation-targeting drug based on afatinib. | |
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V128379 | AFM24 | AFM24 is a bispecific antibody with a TandAb structure, expressed in CHO cells, and targets EGFR and Fcγ-RIIIA. | |
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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. |
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