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编 号:F410180
分子式:C17H10ClFN6
分子量:352.75
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
SD-208 is a selective?TGF-βRI (ALK5)?inhibitor with?IC50?of 48 nM, and > 100-fold selectivity over TGF-βRII.

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).

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 blocks 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.
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