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SD-208

Cat. No. M5038
SD-208 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL In DMSO USD 140 In stock
10mg USD 125 In stock
50mg USD 540 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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).

Customer Product Validations & Biological Datas
Source J Neurosci (2016). Figure 5. SD-208
Method i.p.
Cell Lines EAN rats
Concentrations 20 mg/kg/d
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.
Protocol
Cell Experiment
Cell lines Murine SMA-560 or human LN-308 glioma cells
Preparation method Proliferation.
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).
Concentrations 1 μM
Incubation time 48 h
Animal Experiment
Animal models SMA-560 cells bearing VM/Dk mice
Formulation deionized water
Dosages 1 mg/mL
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 352.75
Formula C17H10ClFN6
CAS Number 627536-09-8
Purity >98%
Solubility DMSO 9 mg/mL warmed
Water <1 mg/mL
Storage at -20°C
References

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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  Catalog
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Keywords: SD-208 supplier, TGF-beta/Smad, inhibitors

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