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氨基酸及其衍生物 抑制剂 常见氨基酸及蛋白质类药
SD-208
发布者:信康   浏览次数:
  • 产品名称:SD-208
  • CAS:627536-09-8
  • 别名:2-(5-氯-2-氟苯基)-N-4-吡啶基-4-蝶啶胺;SD-208;SD208;SD208;SCI208;SD-20810MG;2-(5-氯-2-氟苯基)-4-[(4-吡啶基)氨基]蝶啶
  • 英文名:SD-208
    • 密度 1.487
    • 储存条件 2-8°C
    • 溶解度 DMSO: >5mg/mL
    • 颜色off-white to tan
    • 生物活性SD-208是一种选择性TGF-βRI (ALK5)抑制剂,with IC50为48 nM,选择性比TGF-βRII高100多倍。
    • 体外研究SD-208 inhibits the cell growth and constitutive and TGF-beta-evoked migration and invasion, and enhances immunogenicity in murine SMA-560 and human LN-308 glioma cells. SD-208 blocka TGF-beta-induced phosphorylation of the receptor-associated Smads, Smad2 and Smad3, and stimulates epithelial-to-mesenchymal transdifferentiation, migration, and invasiveness into Matrigel in vitro. SD-208 also abolishes the promoting effect of TGF-β on neointimal smooth muscle-like cell (SMLC) proliferation and migration in vitro.
    • 体内研究SD-208 (1 mg/mL, p.o.) significantly prolongs the median survival of SMA-560 glioma-bearing mice. In syngeneic 129S1 mice, SD-208 (60 mg/kg/d, p.o.) inhibits primary R3T tumor growth, and reduces the number and the size of lung metastases. In the murine aortic allograft model, SD-208 effectively reduces the formation of intimal hyperplasia of transplant arteriosclerosis (TA).