中文名 | SD-208 |
英文名 | SD-208 |
别名 | 化合物SD-208 TGF-ΒRI抑制剂(ALK5抑制剂)(SD-208) 2-(5-氯-2-氟苯基)-N-4-吡啶基-4-蝶啶胺 2-(5-氯-2-氟苯基)-4-[(4-吡啶基)氨基]蝶啶 2-(5-氯-2-氟苯基)-N-(吡啶-4-基)蝶啶-4-胺 |
英文别名 | SD208 SD-208 SD 208 CS-2295 SD-208 (SD 208 TGF-Β RI KINASE INHIBITOR V 2-(5-Chloro-2-fluorophenyl)-4-[(4-pyridyl)amino]pteridine 4-PteridinaMine, 2-(5-chloro-2-fluorophenyl)-N-4-pyridinyl- 2-[(5-CHLORO-2-FLUOROPHENYL)PTERIDIN-4-YL]PYRIDIN-4-YL-AMINE 2-(5-chloro-2-fluorophenyl)-N-(pyridin-4-yl)pteridin-4-amine |
CAS | 627536-09-8 |
化学式 | C17H10ClFN6 |
分子量 | 352.75 |
密度 | 1.487 |
溶解度 | DMSO: >5 mg/mL |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | off-white to tan |
MDL号 | MFCD11519969 |
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. 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.) 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). 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。 |
危险品标志 | Xn - 有害物品 |
风险术语 | 22 - 吞食有害。 |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.835 ml | 14.174 ml | 28.349 ml |
5 mM | 0.567 ml | 2.835 ml | 5.67 ml |
10 mM | 0.283 ml | 1.417 ml | 2.835 ml |
5 mM | 0.057 ml | 0.283 ml | 0.567 ml |
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