Tyrphostin
AG-1024
CAS: 65678-07-1
Molecular Formula: C14H13BrN2O
Tyrphostin - Names and Identifiers
Tyrphostin - Physico-chemical Properties
| Molecular Formula | C14H13BrN2O |
| Molar Mass | 305.17 |
| Solubility | DMSO: soluble |
| Appearance | solid |
| Color | yellow |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| In vitro study | AG-1024 inhibits insulin-like growth factor -1 (IGF-1) and insulin-stimulated cell proliferation with IC50 of 0.4 μm and 0.1 μm, respectively, and inhibits IGF-1 receptor and insulin receptor autophosphorylation, IC50 of 7 μm and 57 μm, respectively, also inhibited the activity of receptor tyrosine kinase on exogenous substrate (TKA), IC50 of 18 μm and 80 μm, respectively. AG-1024 (10 μm) acts on MCF-7 cells and inhibits cell proliferation after 48 hours of treatment. This effect is time-dependent and induces cell apoptosis with an apoptosis rate of 20.1%, when combined with Irradiation (10 Gy), the apoptosis rate was more than 40%, when Irradiation (10 Gy) alone, the apoptosis rate was only 11.8, and the down-regulation of p-Akt1 and bcl-2, and Bax, upregulation of p53 and p21 correlates. In the presence of serum, AG-1024 significantly inhibits the proliferation of malignant melanoma cells by inhibiting the MAPK/ERK2 signaling pathway, followed by rapid induction of pRb dephosphorylation, and finally inhibiting the formation of the pRb-E2F complex, IC50<50 nM. AG-1024 acts on UT7-9 and Ba/F3-p210 cells, down-regulates Bcr-Abl and P-Akt expression, and up-regulates DNA-PKcs expression, resulting in decreased survival and proliferation of cloned genes. AG-1024 also significantly inhibited cell proliferation of the anti-BCR-ABL inhibitor STI571, associated with a dose-dependent decrease in Bcr-Abl protein expression. |
| In vivo study | Consistent with the in vitro anticancer effect of AG-1024, AG-1024 significantly inhibited tumor growth in mice bearing Ba/F3-p210 xenografts at a dose of 30 μg for 10 days. |
Tyrphostin - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
Tyrphostin - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.277 ml | 16.384 ml | 32.769 ml |
| 5 mM | 0.655 ml | 3.277 ml | 6.554 ml |
| 10 mM | 0.328 ml | 1.638 ml | 3.277 ml |
| 5 mM | 0.066 ml | 0.328 ml | 0.655 ml |
Last Update：2024-01-02 23:10:35
Tyrphostin - Reference Information
| biological activity | AG-1024 inhibited autophosphorylation by IGF-1R, with IC50 of 7 μm, with slightly weak effect on IR, the IC50 is 57 μm and specifically distinguishes InsR from IGF-1R (compared to other tyrosine phosphorylation inhibitors). AG-1024 (Tyrphostin, AGS 200) inhibited autophosphorylation by IGF-1R with IC50 of 7 μm, but had a weak effect on IR with IC50 of 57 μm, and specifically distinguish InsR from IGF-1R (compared to other tyrosine phosphorylation inhibitors). |
| Target | Value |
| IGF-1R (NIH-3T3 fibroblasts ) | 7 μM |
| Insulin Receptor (NIH-3T3 fibroblasts ) | 57 μM |
Last Update：2024-04-09 21:32:10
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Product Name: AG-1024 Visit Supplier Webpage Request for quotation
CAS: 65678-07-1
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CAS: 65678-07-1
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