中文同义词:
2-(5-氯-2-氟苯基)-4-[(4-吡啶基)氨基]蝶啶;2-(5-氯-2-氟苯基)-N-4-吡啶基-4-蝶啶胺;TGF-ΒRI抑制剂(ALK5抑制剂)(SD-208)
英文同义词:
SD-208;2-[(5-CHLORO-2-FLUOROPHENYL)PTERIDIN-4-YL]PYRIDIN-4-YL-AMINE;2-(5-Chloro-2-fluorophenyl)-4-[(4-pyridyl)amino]pteridine;2-(5-chloro-2-fluorophenyl)-N-(pyridin-4-yl)pteridin-4-amine;CS-2295;SD-208 (SD 208;SD 208;SD208;TGF-Β RI KINASE INHIBITOR V;4-PteridinaMine, 2-(5-chloro-2-fluorophenyl)-N-4-pyridinyl-
相关类别:
细胞生物学试剂;小分子抑制剂;小分子抑制剂，天然产物;Inhibitors;Smad;TGF-beta
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).
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。
靶点
Target Value
TGF-βRI (ALK5)
(Cell-free assay) 48 nM
TGF-βRI (ALK5)
(Cell-free assay)
48 nM
体外研究
在小鼠SMA-560和人SMA-560胶质瘤细胞中，SD-208抑制细胞生长，组成，和TGF-β诱发的迁移和浸润，并增强免疫原性。在体外，SD-208阻断TGF-β诱导的受体相关的Smads，Smad2和Smad3磷酸化，并刺激上皮细胞到间叶细胞的分化转化，迁移，以及侵袭到基底膜。在体外，SD-208也会废除TGF-β对新生内膜平滑肌样细胞(SMLC)增殖和迁移的保护作用。
体内研究
SD-208 (1 mg/mL, p.o.)显著延长负荷SMA-560胶质瘤小鼠的中值存活率。在同源129S1小鼠体内，SD-208 (60 mg/kg/d, p.o.)抑制初级R3T肿瘤生长，并减少肺转移的数量和大小。在小鼠大动脉同种移植模型中，SD-208有效减少移植动脉硬化(TA)内膜增生的形成。
