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化學性質:
規格 | 1mg 5mg 10mg 25mg |
CAS | 7 |
別名 | NSC 380341,Tyrphostin AG-1295 |
化學名 | 6,7-dimethyl-2-phenyl-quinoxaline |
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 |
儲存條件 | Store at -20°C |
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 |
產品描述:
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.
特別提醒:
1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療,食品及化妝品等用途。請勿存放于普通住宅區。
2. 為了您的安全和健康,請穿好實驗服并佩戴一次性手套和口罩操作。
原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278