| CAS NO: | 71897-07-9 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 71897-07-9 |
| 别名 | 酪氨酸磷酸化抑制剂AG1295,NSC 380341,Tyrphostin AG-1295 |
| 化学名 | 6,7-dimethyl-2-phenyl-quinoxaline |
| Canonical SMILES | CC1=CC2=NC=C(N=C2C=C1C)C3=CC=CC=C3 |
| 分子式 | C16H14N2 |
| 分子量 | 234.3 |
| 溶解度 | ≤5mg/ml in ethanol;2mg/ml in DMSO;2.5mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50: 0.3-1 μM for PDGF receptor kinase in vitro and in Swiss 3T3 cells AG-1295 is a potent and selective inhibitor of PDGF receptor kinase. Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. PTK inhibitors specific for platelet-derived growth factor (PDGF) receptor kinase could help in the treatment of restenosis, pulmonary fibrosis, atherosclerosis and gliomas. In vitro: The previous study investigated the effect of PDGF receptor-beta (PDGFR-β) inhibition by AG-1295 on the osteogenic differentiation of the mouse pre-osteoblastic cell line MC3T3-E1. Results showed that AG-1295 could significantly increase the alkaline phosphatase (ALP) activity and enhance the formation of mineralized nodules dose-dependently. Moreover, the treatment with AG-1295 led to the up-regulated mRNA expression of the osteogenic marker genes collagen type I, runt-related transcription factor 2, osterix, tissue-nonspecific alkaline phosphatase, as well as osteocalcin. Consistent with its effect on osteoblast differentiation, AG-1295 was also able to significantly suppress the phosphorylation of Erk1/2 in MC3T3-E1 cells [1]. In vivo: A previous animal study was designed to evaluated the possible effects of AG1295 on the development of interstitial fibrosis in rats with unilateral ureteral obstruction, monitored by ED-A+ fibronectin expression, the number of macrophages. Results showed that the i.p.treatment with AG1295 at 12 mg/kg could significantly reduce interstitial fibrosis as verified by a smaller Sirius-Red stained area and also by a reduced number of macrophages, and by the ED-A+ fibronectin deposition and the number of cells positive for α-smooth muscle actin [2]. Clinical trial: So far, no clinical study has been conducted. References: |
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