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SD-208
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SD-208图片
CAS NO:627536-09-8
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)352.75
FormulaC17H10ClFN6
CAS No.627536-09-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 9 mg/mL (25.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)1% methylcellulose: 8 mg/mL
Synonyms

SD-208; SD 208; TGF-β RI Kinase Inhibitor V; SD208;

Chemical Name: 2-(5-chloro-2-fluorophenyl)-N-4-pyridinyl-4-pteridinamine

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

Exact Mass: 352.064

实验参考方法
In Vitro

In vitro activity: 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 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. SD-208 also abolishes the promoting effect of TGF-β on neointimal smooth muscle-like cell (SMLC) proliferation and migration in vitro.


Kinase Assay: 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.


Cell Assay: 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.

In VivoSD-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).
Animal modelVM/Dk mice bearing SMA-560 tumors
Formulation & DosageDissolved in water; 1 mg/mL; p.o.
References

Cancer Res. 2004 Nov 1;64(21):7954-61; Clin Cancer Res. 2006 Jul 15;12(14 Pt 1):4315-30.