产品说明书

PF-8380

Print
Chemical Structure| 1144035-53-9 同义名 : -
CAS号 : 1144035-53-9
货号 : A244971
分子式 : C22H21Cl2N3O5
纯度 : 99%+
分子量 : 478.325
MDL号 : MFCD20527274
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(219.52 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

1%CMC Na +water 15 mg/mL suspension

生物活性
靶点

  • PDE

    Autotaxin, IC50:2.8 nM
描述 PF-8380 inhibits rat autotaxin with an IC50 of 1.16 nM when tested with the FS-3 substrate. The efficacy of PF-8380 is sustained when the enzyme, derived from fetal fibroblasts, is combined with lysophosphatidyl choline (LPC) as the substrate. In human whole blood incubated with PF-8380 for 2 hours, autotaxin inhibition occurs with an IC50 of 101 nM[1]. Autotaxin (ATX), an enzyme with lysophospholipase D (lysoPLD) activity, converts lysophosphatidylcholine (LPC) into lysophosphatidic acid (LPA). Treatment of GL261 and U87-MG cells with 1 μM PF-8380 prior to 4 Gy irradiation leads to reduced clonogenic survival, lowered migration (33% in GL261; P=0.002 and 17.9% in U87-MG; P=0.012), decreased invasion (35.6% in GL261; P=0.0037 and 31.8% in U87-MG; P=0.002), and reduced radiation-induced Akt phosphorylation[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.45mL

2.09mL

1.05mL

20.91mL

4.18mL

2.09mL
参考文献

[1]Gierse J, et al. A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation. J Pharmacol Exp Ther. 2010 Jul;334(1):310-7.

[2]Bhave SR, et al. Autotaxin Inhibition with PF-8380 Enhances the Radiosensitivity of Human and Murine Glioblastoma Cell Lines. Front Oncol. 2013 Sep 17;3:236.