Research Area
Product Type
United States ( Change Country )
AG-1478 (Tyrphostin AG-1478) Chemical Structure
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Biological Activity
AG-1478 (Tyrphostin AG-1478) is a highly potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with an IC50 of 3 nM. Much higher concentrations are required for AG-1478’s prevention of the kinase activity of the closely-related HER2(neu/erbB2) receptor (IC50> 100 μM), the platelet-derived growth factor receptor (PDGFR) with IC50>100 μM), and p210Bcr-Abl (IC50 > 5 0 μM). That AG-1478 (Tyrphostin AG-1478) has been used in a broad range of studies contributes to its potency and selectivity. AG-1478 (Tyrphostin AG-1478) reversibly prevents rat brain Kv1.5 potassium channels (IC50 = 9.8 µM) independent of PTK activity. Additionally, AG-1478 (Tyrphostin AG-1478) also suppresses the growth of leiomyoma and myometrium cell cultures with IC50 values of 5.6 and 5.7 µM, respectively. AG-1478 (Tyrphostin AG-1478) blocke the activation of MAP kinase and strongly represses induction of fos gene expression and DNA synthesis. AG-1478 (Tyrphostin AG-1478) promotes optic nerve regeneration. [1] AG-1478 (Tyrphostin AG-1478) enhances expression of pSAPK/JNK, while selective JNK inhibitor SP 600125 elevates expression of GSK-3β (S9P). The selective EGFR inhibitor AG-1478 (Tyrphostin AG-1478) are observed to be able to block EGFR-mediated signaling pathway and prevent versican G3 induced effects on mammary cancer cell proliferation. In particular, versican G3 enhanced cell survival is prevented by selective EGFR inhibitor AG-1478 (Tyrphostin AG-1478) through mechanisms blocking G3 activated expression of pERK and GSK-3 β (S9P). AG-1478 (Tyrphostin AG-1478) blocks G3 enhanced effects on cell apoptosis. [2] AG-1478 (Tyrphostin AG-1478) is active both in vitro in cell lines such as colon cancer, non-small cell lung cancer and glioblastoma cell models and in vivo in mice xenograft models. In tumor xenograft models AG-1478 (Tyrphostin AG-1478) prevents the growth of A431 tumors and human glioblastomas which over-express a mutant EGFR. [3]
References on AG-1478 (Tyrphostin AG-1478)
- [1] ACS Nano. 2011;5(6), 4392-4400
- [2] PLoS One. 2011;6(11), e26396
- [3] Biochem Pharmacol. 2006;71(10), 1422-34
Chemical Information
| Molecular Weight (WM): | 315.75 |
|---|---|
| Formula: | C16H14ClN3O2 |
| CAS No.: | 153436-53-4 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥63mg/mL |
| Water <1mg/mL | |
| Ethanol ≥13mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
View current batch:
Research Area
Receptor Tyrosine Kinase >> EGFR >> EGFR Inhibitors
Angiogenesis >> EGFR >> EGFR Inhibitors
JAK / STAT >> EGFR >> EGFR Inhibitors
Angiogenesis >> EGFR >> EGFR Inhibitors
JAK / STAT >> EGFR >> EGFR Inhibitors
Notes:
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Selleck's high quality products have been used in several published research findings, including the following:
MECHANISMS AND ANALYSIS OF THE CNS DISTRIBUTION OF CEDIRANIB,A MOLECULARLY-TARGETED ANTI-ANGIOGENIC AGENT
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