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抑制剂描述:

产品名称:PF-8380

产品别名:见爱必信官网

英文别名:PF-8380

靶点:PDE

CAS:1144035-53-9

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

PF-8380 is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood. 

溶解性:DMSO : ≥ 56 mg/mL (117.07 mM)

体外研究:

PF-8380 inhibits rat autotaxin with an IC50 of 1.16 nM with FS-3 substrate. In human whole blood incubated with compound for 2 h autotaxin was inhibited with an IC50 of 101 nM.Inhibition of autotaxin by PF-8380 leads to decreased invasion, migtation and enhanced radiosensitization of GBM cells. Radiation-induced activation of Akt is abrogated by inhibition of ATX. Furthermore, inhibition of ATX leads to diminished tumor vascularity and delayed tumor growth.

体内研究:Pre-treatment with PF-8380 prior to irradiation inhibited radiation-induced angiogenesis of tumor vascular endothelial cells and delayed progression of glioma tumor growth in vivo. Oral administration of 30 mg/kg PF8380 reduces inflammatory hyperalgesia in a rat air pouch model, exhibiting >95% reduction of LPA levels in both plasma and inflammatory site tissue within 3 hours.

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