AG-1295
(Synonyms: 酪氨酸磷酸化抑制剂AG1295,NSC 380341,Tyrphostin AG-1295) 目录号 : GC16235
A selective inhibitor of PDGF receptor kinase
Cas No.:71897-07-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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:
[1] Zhang YY, Cui YZ, Luan J, Zhou XY, Zhang GL, Han JX. Platelet-derived growth factor receptor kinase inhibitor AG-1295 promotes osteoblast differentiation in MC3T3-E1 cells via the Erk pathway. Biosci Trends. 2012 Jun;6(3):130-5.
[2] Ludewig D, Kosmehl H, Sommer M, Bhmer FD, Stein G. PDGF receptor kinase blocker AG1295 attenuates interstitial fibrosis in rat kidney after unilateral obstruction. Cell Tissue Res. 2000 Jan;299(1):97-103.
| Cas No. | 71897-07-9 | SDF | |
| 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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.268 mL | 21.3402 mL | 42.6803 mL |
| 5 mM | 0.8536 mL | 4.268 mL | 8.5361 mL |
| 10 mM | 0.4268 mL | 2.134 mL | 4.268 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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