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产品介绍
产品介绍
产品信息
抗原名称
Autotaxin
商品描述
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.
分子量
478.33
纯度
＞98%
可溶性
DMSO : ≥ 56 mg/mL (117.07 mM)
外观
white to beige powder
In vitro(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.
In vivo(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.
背景
别名
PF 8380
分子式
C22H21Cl2N3O5
CAS号
1144035-53-9
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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