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PF-04802367

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Chemical Structure| 1962178-27-3 同义名 : PF-367
CAS号 : 1962178-27-3
货号 : A1398967
分子式 : C16H16ClN5O3
纯度 : 98%
分子量 : 361.783
MDL号 : MFCD30146406
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(290.23 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：
生物活性
描述 PF-04802367 is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM in the recombinant human GSK-3β enzyme assay and 1.1 nM in the ADP-Glo assay. PF-04802367 inhibits the two known GSK-3 isoforms, GSK-3α and GSK-3β, with identical IC50 values in mobility shift assays. The IC50 values of PF-04802367 were 10.0 and 9.0 nM in the mobility shift assay, respectively. PF-04802367 has reasonable in vitro stability in human liver microsomes (t1/2=78.7 min) and excellent passive permeability. In a stably induced CHO cell line overexpressing GSK-3β and its substrate tau, PF-04802367 inhibited tau phosphorylation with an IC50 of 466 nM[1].PF-04802367 had a significant right-shifting effect on β-catenin translocation in HeLa cells (EC50 of 6.2 μM), gene transcription in U20S cells (EC50 of 20.6 μM) and cell proliferation in HeLa cells (EC50 of 9.0 μM)[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.76mL

0.55mL

0.28mL

13.82mL

2.76mL

1.38mL

27.64mL

5.53mL

2.76mL
参考文献

[1]Steven H Liang, et al. Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging. Angew Chem Int Ed Engl. 2016 Aug 8;55(33):9601-5.

[2]Vadim Bernard-Gauthier, et al. Structural Basis for Achieving GSK-3β Inhibition with High Potency, Selectivity, and Brain Exposure for Positron Emission Tomography Imaging and Drug Discovery. J Med Chem. 2019 Nov 14;62(21):9600-9617.