SD-208

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SD-208 是一种有效的选择性 TGF-β 受体 I 激酶 (TGF-βRI) 抑制剂，IC50 为 48 nM。

SD-208 is a potent, selective TGF-β receptor I kinase (TGF-βRI) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII kinase and >20-fold over a panel of related protein kinases; inhibits the growth inhibition of TGF-beta-sensitive CCL64 cells mediated by recombinant TGF-β1 or TGF-β2 or of TGF-β-containing glioma cell supernatant with EC50 of 0.1 uM; inhibits constitutive and TGF-β–induced invasion of glioma cells, inhibits TGF-β signaling in immune effector cells; blocks TGF-β signaling in the brain and inhibits the growth of syngeneic SMA-560 experimental gliomas in vivo.

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.

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).

SD 208 | SD208

TGF-beta/Smad

TGFBR

TGF-βRI(ALK5)

Cancer

——

627536-09-8

352.7529

C17H10ClFN6

>98% (HPLC)

10 mM in DMSO

FC1=CC=C(Cl)C=C1C2=NC(NC3=CC=NC=C3)=C4N=CC=NC4=N2

4-Pteridinamine, 2-(5-chloro-2-fluorophenyl)-N-4-pyridinyl-

(-20℃)

With Ice Pack

≥ 2 years