酪氨酸磷酸化抑制剂AG1295
- CAS号:71897-07-9
- 英文名:AG 1295
- 中文名:酪氨酸磷酸化抑制剂AG1295
- CBNumber:CB5683675
- 分子式:C16H14N2
- 分子量:234.3
- MOL File:71897-07-9.mol
- 熔点 :121 °C
- 沸点 :398.3±37.0 °C(Predicted)
- 密度 :1.127±0.06 g/cm3(Predicted)
- 储存条件 :−20°C
- 溶解度 :Chloroform (Slightly), Ethyl Acetate (Slightly)
- 形态 :White solid
- 酸度系数(pKa) :1.29±0.30(Predicted)
- 颜色 :Yellow
- 安全说明 :22-24/25
- WGK Germany :3
酪氨酸磷酸化抑制剂AG1295性质、用途与生产工艺
- 生物活性 AG 1295 是一种选择性血小板衍生生长因子受体 (PDGFR) 酪氨酸激酶抑制剂。AG1295 能抑制 PDGFR 的自磷酸化，对 EGF 受体的自磷酸化无效。
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靶点
PDGFR
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体外研究
AG 1295 inhibits PDGFR autophosphorylation with IC 50 s of 0.3-0.5 μM and 0.5-1 μM for membrane autophosphorylation assays and Swiss 3T3 cells, respectively.
AG1295 (10 μM, 100 μM) significantly inhibits rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB in vitro.
Cell Viability Assay
Cell Line: Rabbit conjunctival fibroblasts cells Concentration: 1 μM, 10 μM, 100 μM Incubation Time: 3 days Result: Inhibited rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB. -
体内研究
AG-1295 reduces neointimal formation in aortic allograft vasculopathy by inhibition of PDGFR-beta-triggered tyrosine phosphorylation.
AG1295 (12 mg/kg; i.p.; daily; for 14 or 21 days) significantly reduces 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 alpha-smooth muscle actin.
Animal Model: Sprague-Dawley rats (240-270 g) Dosage: 12 mg/kg Administration: Intraperitoneal injection; daily; for 14 or 21 days Result: Attenuated interstitial fibrosis in rat kidney after unilateral obstruction.
- 更新日期：2024/04/30
- 产品编号：HY-101957
- 产品名称：酪氨酸磷酸化抑制剂AG1295 AG 1295
- CAS编号：71897-07-9
- 包装：5mg
- 价格：600元
- 更新日期：2024/04/30
- 产品编号：HY-101957
- 产品名称：酪氨酸磷酸化抑制剂AG1295 AG 1295
- CAS编号：71897-07-9
- 包装：10mM * 1mLin DMSO
- 价格：660元
- 公司名称：SIGMA
- 联系电话：--
- 电子邮件：
- 国家：瑞士
- 产品数：6913
- 优势度：91
- 公司名称：ALEXIS
- 联系电话：--
- 电子邮件：alexis-ch@alexis-corp.ch
- 国家：瑞士
- 产品数：3599
- 优势度：74
