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SD-208

SKU: orb1224418

Description

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.

Images & Validation

Key Properties

CAS Number627536-09-8
MW352.7529
Purity>98% (HPLC)
FormulaC17H10ClFN6
SMILESFC1=CC=C(Cl)C=C1C2=NC(NC3=CC=NC=C3)=C4N=CC=NC4=N2
TargetTGFBR
Solubility10 mM in DMSO

Bioactivity

In Vivo
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).
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. 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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SD 208 | SD208

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Protocol Information

SD-208 (orb1224418)

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Available Sizes

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200 mg
500 mg
2 mg
¥ 1,170.00
5 mg
¥ 1,690.00
10 mg
¥ 2,080.00
25 mg
¥ 4,030.00
50 mg
¥ 5,850.00
100 mg
¥ 8,840.00