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生物活性
XAV-939 was screened out as an inhibitor of Wnt/β-catenin pathway. In HEK293 cells, XAV-939 significantly inhibited the Wnt3a-stimulated STF activity and β-catenin accumulation. In SW480 cells, XAV-939 also inhibited STF activity and increased β-catenin phosphorylation. XAV-939 was demonstrated to stabilize the axin levels through inhibiting tankyrases and subsequently inhibit the Wnt signaling. It tightly bound to the catalytic domains of tankyrase 1 and tankyrase 2 with Kd values of 99 and 93 nM, respectively. In addition, XAV-939 significantly inhibited colony formation of β-catenin-dependent DLD-1 cells but not β-catenin-independent RKO cells.
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体外研究
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体内研究
30% PEG400+0.5% Tween80+5% Propylene glycol
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激酶实验
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细胞实验
1.0 μM
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动物实验
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不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
[1] Dregalla RC, et al. Aging, 2010, 2(10), 691-708.
[2] Smith, S., et al., 1998. Tankyrase, a poly(ADP-ribose) polymerase at human telomeres. Science (New York, N.Y.). 282(5393): 1484-7.
[3] Huang, Shih-Min A., et al., 2009. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 461(7264): 614-20.
分子式
C14H11F3N2OS |
分子量
312.3 |
CAS号
284028-89-3 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
|
DMSO
5 mg/mL |
Water
<1 mg/mL |
Ethanol
<1 mg/mL |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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