Molecular Formula | C17H10ClFN6 |
Molar Mass | 352.75 |
Density | 1.487 |
Solubility | DMSO: >5mg/mL |
Appearance | powder |
Color | off-white to tan |
Storage Condition | 2-8°C |
MDL | MFCD11519969 |
Use | SD-208 |
In vitro study | 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. In Mouse SMA-560 and human SMA-560 glioma cells, SD-208 inhibited cell growth, composition, and TGF-β-induced migration and infiltration, and enhanced immunogenicity. In vitro, SD-208 blocked TGF-β-induced receptor-associated Smads,Smad2 and Smad3 phosphorylation and stimulated differentiation and transformation of epithelial cells into mesenchymal cells, migration, and invasion to the basement membrane. SD-208 also abrogated the protective effect of TGF-β on neointimal smooth muscle-like cell (SMLC) proliferation and migration in vitro. |
In vivo study | 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 effective reduction the formation of implicit hyperasia of transpolant arthritis (TA). SD-208 (1 mg/ml, p.o.) significantly prolonged the median survival of SMA-560 glioma-bearing mice. In homologous 129S1 mice, SD-208 (60 mg/kg/d, p.o.) inhibited primary R3T tumor growth and reduced the number and size of lung metastases. In the large artery allograft model of mice, SD-208 effectively reduced the formation of intimal hyperplasia in transplant arteriosclerosis (TA). |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
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 |
biological activity | SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, which is more than 100 times higher than βTGF-RII. SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, which is more than 100 times higher than TGF-βRII. |
in vitro study | 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 blockka 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. in mouse SMA-560 and human SMA-560 glioma cells, SD-208 inhibit cell growth, composition, and TGF-β-induced migration and infiltration, and enhance immunogenicity. In vitro, SD-208 blocks TGF-β-induced receptor-related Smads,Smad2, and Smad3 phosphorylation and stimulates epithelial-to-mesenchymal differentiation transformation, migration, and invasion to the basement membrane. In vitro, SD-208 will also abolish the protective effect of TGF-β on the proliferation and migration of neointimal smooth muscle-like cells (SMLC). |
in vivo study | 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 auric allograft model, SD-208 effectively reduces the formation of intimal hyperplasia of transplant arteriosclerosis (TA). SD-208 (1 mg/mL, p.o.) significantly prolonged the median survival rate of mice loaded with SMA-560 glioma. In homologous 129S1 mice, SD-208 (60 mg/kg/d, p.o.) inhibited primary R3T tumor growth and reduced the number and size of lung metastases. In the mouse large artery allograft model, SD-208 effectively reduce the formation of intimal hyperplasia of transplanted arteriosclerosis (TA). |
target | TargetValue TGF-βRI (ALK5) (Cell-free say) 48 nM |
Target | Value |
TGF-βRI (ALK5) (Cell-free assay) | 48 nM |