酪氨酸磷酸化抑制剂AG1295
酪氨酸磷酸化抑制剂AG1295 性质
| 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 | 氯仿（微溶）、乙酸乙酯（微溶） |
| 酸度系数(pKa) | 1.29±0.30(Predicted) |
| 形态 | 白色固体 |
| 颜色 | 粘黄色 |
| InChI | 1S/C16H14N2/c1-11-8-14-15(9-12(11)2)18-16(10-17-14)13-6-4-3-5-7-13/h3-10H,1-2H3 |
| InChIKey | FQNCLVJEQCJWSU-UHFFFAOYSA-N |
| SMILES | n1c2c(ncc1c3ccccc3)cc(c(c2)C)C |
酪氨酸磷酸化抑制剂AG1295 用途与合成方法
PDGFR
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. |
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. |
酪氨酸磷酸化抑制剂AG1295 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026-06-05 | HY-101957R | 酪氨酸磷酸化抑制剂AG1295 | 71897-07-9 | 5 mg | 1250 |
| 2026-06-05 | HY-101957R | 酪氨酸磷酸化抑制剂AG1295 | 71897-07-9 | 10 mg | 2000 |
