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SD208

(CAS No:627536-09-8)
SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
CAS No:627536-09-8
Molecular Weight(MW):352.75
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 627536-09-8
Molecular formula(MF) C17H10ClFN6
Molecular Weight(MW): 352.75
Alias
Solubility
In vitro DMSO 9 mg/mL warmed (25.51 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% methylcellulose 8mg/mL
Biological Activity
Description SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
Targets
TGF-βRI (ALK5) [1]
48 nM
In vitro

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. [1] 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. [2] SD-208 also abolishes the promoting effect of TGF-β on neointimal smooth muscle-like cell (SMLC) proliferation and migration in vitro. [3]

In vivo SD-208 (1 mg/mL, p.o.) significantly prolongs the median survival of SMA-560 glioma-bearing mice. [1] 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. [2] In the murine aortic allograft model, SD-208 effectively reduces the formation of intimal hyperplasia of transplant arteriosclerosis (TA). [3]