1. TGF-beta/Smad
  2. TGF-β Receptor

SD-208 

Cat. No.: HY-13227 Purity: 98.33%
Handling Instructions

SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.

For research use only. We do not sell to patients.

SD-208 Chemical Structure

SD-208 Chemical Structure

CAS No. : 627536-09-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 164 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 149 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 629 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.

IC50 & Target

IC50: 48 nM (TGF-βRI)

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-β 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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8349 mL 14.1743 mL 28.3487 mL
5 mM 0.5670 mL 2.8349 mL 5.6697 mL
10 mM 0.2835 mL 1.4174 mL 2.8349 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Various kinase activities are assayed by measuring the incorporation of radiolabeled ATP into a peptide or protein substrate. The reactions are performed in 96-well plates and included the relevant kinase, substrate, ATP, and appropriate cofactors. The reactions are incubated and then stopped by the addition of phosphoric acid. Substrate is captured onto a phosphocellulose filter, which is washed free of unreacted ATP. The counts incorporated are determined by counting on a microplate scintillation counter. The ability of SD-208 to inhibit the respective kinase is determined by comparing counts incorporated in the presence of compound with those incorporated in the absence of compound.

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

Cell Assay
[1]

Glioma cells are cultured in the absence or presence of SD-208 (1 μM) for 48 hours. The cells are pulsed for the last 24 hours with [methyl-3H]thymidine (0.5 μCi) and harvested, and incorporated radioactivity is determined in a liquid scintillation counter.

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

Animal Administration
[1]

VM/Dk mice are purchased from the TSE Resource Center. Mice of 6 to 12 weeks of age are used for the survival experiments. Groups of eight mice are anesthesized before all intracranial procedures and placed in a stereotaxic fixation device. A burr hole is drilled in the skull 2 mm lateral to the bregma. The needle of a Hamilton syringe is introduced to a depth of 3 mm. SMA-560 cells [5×103cells] resuspended in a volume of 2 μL of PBS are injected into the right striatum. Three days later, the mice are allowed to drink SD-208 at 1 mg/mL in deionized water. The mice are observed daily and, in the survival experiments, sacrificed on development of neurologic symptoms.

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

References
Molecular Weight

352.75

Formula

C₁₇H₁₀ClFN₆

CAS No.

627536-09-8

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SD-208
Cat. No.:
HY-13227
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SD-208

Cat. No.: HY-13227