153436-53-4
4-(3-Chloroanilino)-6,7-Dimethoxyquinazoline Hydrochloride
CAS: 153436-53-4
Molecular Formula: C16H14ClN3O2
153436-53-4 - Names and Identifiers
153436-53-4 - Physico-chemical Properties
| Molecular Formula | C16H14ClN3O2 |
| Molar Mass | 315.75 |
| Density | 1.337 |
| Melting Point | 247 °C(dec.) |
| Boling Point | 458.5±45.0 °C(Predicted) |
| Appearance | White to light yellow solid. |
| Maximum wavelength(λmax) | 332nm(lit.) |
| pKa | 5.54±0.30(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
| In vitro study | AG-1478 was less selective for ErbB2 and PDGFR with an IC50 of> 100 μm. AG -34.6 preferentially inhibits Δegfr-expressing U87MG cells compared to cells expressing endogenous wt EGFR or over-expressing exogenous wt EGFR (IC50 48.4 μm and 1478 μm, respectively), the IC50 was 8.7 μm, and inhibited DNA synthesis with an IC50 of 4.6 μm, 19.67 μm, and 35.2 μm, respectively. AG-1478 also preferentially inhibits tyrosine kinase activity and the autophosphorylation of Δegfr compared to endogenous or overexpressed exogenous wt EGFR. In VSMC, AG-1478 (0.25 μm) abolished Ang II,Ca2 ionophore and EGF-induced MAPK activation, however, it did not affect the MAPK activation induced by phorbol ester or platelet-derived growth factor-BB. AG-1478 inhibited EGF-induced mitosis in BaF/ERX and LIM1215 cells with an IC50 of 0.07 μm and 0.2 μm, respectively. AG1478 can inhibit the function of ATP-binding cassette (ABC) transporters, such as ABCB1 and ABCG2, and has a significant effect on ABCG2. |
| In vivo study | AG-1478 administration blocked EGFR phosphorylation at tumor sites and inhibited the growth of A431 xenografts overexpressing wt EGFR and glioma xenografts expressing de2-7 EGFR. Even an insufficient therapeutic dose of AG-1478 can significantly enhance the efficacy of cytotoxic drugs, showing synergistic antitumor activity in combination with AG-1478 and temozoloride on human glioma xenografts. AG-1478 binding anti-EGFR antibody (mAb 806) exhibits additional, in some cases synergistic, anti-tumor activity on EGFR overexpressing tumor xenografts. AG-1478 (0.4 mg) combined with a single dose of 25 μCi |
153436-53-4 - Risk and Safety
| RTECS | VA0953000 |
| HS Code | 29339900 |
153436-53-4 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.839 ml | 14.196 ml | 28.393 ml |
| 5 mM | 0.568 ml | 2.839 ml | 5.679 ml |
| 10 mM | 0.284 ml | 1.42 ml | 2.839 ml |
| 5 mM | 0.057 ml | 0.284 ml | 0.568 ml |
Last Update：2024-01-02 23:10:35
153436-53-4 - Introduction
AG-1478, also known as Tyrphostin AG-1478, is a tyrosine kinase inhibitor. Its chemical name is 4-(3-chlorine aniline)-6,7-dimethoxyquinazoline, the chemical formula is C16H14ClN3O2, and the relative molecular mass is 315.8.
AG-1478 is primarily used as an inhibitor of the epidermal growth factor receptor (EGFR). EGFR is a receptor-type tyrosine kinase involved in the regulation of cell growth, differentiation, and survival. AG-1478 can bind to the tyrosine kinase activity of EGFR, inhibit its phosphorylation and downstream signal transduction, thereby inhibiting cell proliferation. Therefore, AG-1478 is widely used in cancer research, especially for the treatment of EGFR-overexpressing tumors.
The preparation of AG-1478 is mainly obtained by chemical synthesis. Specific synthetic methods can be referred to the relevant chemical literature.
When using AG-1478, pay attention to the following safety information:
1. AG-1478 is an organic compound and should avoid contact with skin and inhalation of its dust or gas. Wear appropriate protective equipment such as gloves and masks when operating.
2. AG-1478 may cause irritation and damage to the eyes and respiratory system, so avoid touching the eyes or inhaling it during operation.
3. AG-1478 should be stored in a dry, cool place, avoid direct sunlight.
4. For the specific use and handling of AG-1478, please follow the safety operation procedures of relevant chemicals and MSDS (chemical safety technical instructions). When using, please consult the relevant literature and the guidance of relevant professionals.
AG-1478 is primarily used as an inhibitor of the epidermal growth factor receptor (EGFR). EGFR is a receptor-type tyrosine kinase involved in the regulation of cell growth, differentiation, and survival. AG-1478 can bind to the tyrosine kinase activity of EGFR, inhibit its phosphorylation and downstream signal transduction, thereby inhibiting cell proliferation. Therefore, AG-1478 is widely used in cancer research, especially for the treatment of EGFR-overexpressing tumors.
The preparation of AG-1478 is mainly obtained by chemical synthesis. Specific synthetic methods can be referred to the relevant chemical literature.
When using AG-1478, pay attention to the following safety information:
1. AG-1478 is an organic compound and should avoid contact with skin and inhalation of its dust or gas. Wear appropriate protective equipment such as gloves and masks when operating.
2. AG-1478 may cause irritation and damage to the eyes and respiratory system, so avoid touching the eyes or inhaling it during operation.
3. AG-1478 should be stored in a dry, cool place, avoid direct sunlight.
4. For the specific use and handling of AG-1478, please follow the safety operation procedures of relevant chemicals and MSDS (chemical safety technical instructions). When using, please consult the relevant literature and the guidance of relevant professionals.
Last Update：2024-04-10 22:29:15
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