SD-208 

SD-208 (GMP) is SD-208 (HY-13227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC₅₀ of 48 nM, and > 100-fold selectivity over TGF-βRII.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SD-208 (GMP) (1 mg/mL, p.o.) significantly prolongs the median survival of SMA-560 glioma-bearing mice^[1].
In syngeneic 129S1 mice, SD-208 (GMP) (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 (GMP) effectively reduces the formation of intimal hyperplasia of transplant arteriosclerosis (TA)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

352.75

C₁₇H₁₀ClFN₆

627536-09-8

FC1=CC=C(Cl)C=C1C2=NC3=NC=CN=C3C(NC4=CC=NC=C4)=N2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Uhl M, et al. SD-208, a novel transforming growth factor beta receptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo. Cancer Res. 2004 Nov 1;64(21):7954-61.  [Content Brief]

  [2]. Ge R, et al. Inhibition of growth and metastasis of mouse mammary carcinoma by selective inhibitor of transforming growth factor-beta type I receptor kinase in vivo. Clin Cancer Res. 2006 Jul 15;12(14 Pt 1):4315-30.  [Content Brief]

  [3]. Sun Y, et al. Inhibition of intimal hyperplasia in murine aortic allografts by the oral administration of the transforming growth factor-beta receptor I kinase inhibitor SD-208. J Heart Lung Transplant. 2014 Jun;33(6):654-61.  [Content Brief]