SD-208

627536-09-8

C17H10ClFN6

DMSO : 9.09 mg/mL (25.77 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

TGF-beta/Smad

SD-208 is a selective TGF-betaRI (ALK5) inhibitor with IC₅₀ of 48 nM, and > 100-fold selectivity over TGF-betaRII. IC50 & Target: IC50: 48 nM (TGF-betaRI) 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 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^[2]. SD-208 also abolishes the promoting effect of TGF-beta 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].