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.In the murine aortic allograft model, SD-208 effectively reduces the formation of intimal hyperplasia of transplant arteriosclerosis (TA).
|Cell lines||Murine SMA-560 or human LN-308 glioma cells|
Glioma cells were cultured in the absence or presence of SD-208 (1 μmol/L) for 48 hours. The cells were pulsed for the last 24 hours with [methyl-3H]thymidine (0.5 μCi) and harvested (Tomtec, Hamden, CT), and incorporated radioactivity was determined in a liquid scintillation counter (Wallac, Turku, Finland).
|Incubation time||48 h|
|Animal models||SMA-560 cells bearing VM/Dk mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 9 mg/mL warmed;Water <1 mg/mL|
|Source||J Neurosci (2016). Figure 5. SD-208|
|Cell Lines||EAN rats|
|Incubation Time||12 day|
|Results||In both the SD-208 alone and RvD1 + SD-208 groups, EAN rats showed much more severe neurological scores and significantly prolonged disease duration, not only compared with the RvD1 + vehicle group, but also compared with the vehicle-alone group (Fig. 5B), suggesting that the inhibition of TGF-β signaling not only abolished the exogenous RvD1 effects, but also may suppress endogenous RvD1 functions.|
Inhibition of intimal hyperplasia in murine aortic allografts by the oral administration of the transforming growth factor-beta receptor I kinase inhibitor SD-208.
Sun Y,et.al. J Heart Lung Transplant. 2014 Jun;654-61. PMID: 24685405.
Inhibition of growth and metastasis of mouse mammary carcinoma by selective inhibitor of transforming growth factor-beta type I receptor kinase in vivo.
Ge R,et.al. Clin Cancer Res. 2006 Jul 15;4315-30. PMID: 16857807.
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.
Uhl M, et al. Cancer Res. 2004 Nov 1;64(21):7954-61. PMID: 15520202.
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