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GNF-6231
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GNF-6231图片
CAS NO:1243244-74-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)448.49
FormulaC24H25FN6O2
CAS No.1243245-18-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 90 mg/mL
Water: 5 mg/mL
Ethanol: < 1 mg/mL
Chemical Name N-(5-(4-acetylpiperazin-1-yl)pyridin-2-yl)-2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)acetamide
Synonyms GNF6231; GNF 6231; GNF-6231
SMILES Code O=C(NC1=NC=C(N2CCN(C(C)=O)CC2)C=C1)CC3=CN=C(C4=CC(F)=NC=C4)C(C)=C3
实验参考方法
In Vitro

In vitro activity: As an orally active and selective Porcupine inhibitor, GNF-6231 has no appreciable activities, at least up to 10 μM testing concentrations, for more than 200 off-targets, which include GPCRs, kinases, proteases, transporters, ion channels, and nuclear receptors. GNF-6231 shows IC50s of greater than 10 μM on all CYP isoforms tested (2C9, 2D6, 3A4). It shows high permeability in a Caco-2 human cell permeability assay with a possible efflux.


Kinase Assay: GNF-6231 is a potent and selective Porcupine inhibitor with an IC50 of 0.8 nM.


Cell Assay: the TM3 Wnt-Luc and L-cell Wnt3A cells are co-cultured in a 384-well plate with DMEM supplemented with 2% (vol/vol) FBS and treated with different concentrations of compounds. After 24 h, the firefly luciferase activities are assayed with the Bright-Glo Luciferase Assay System. The IC50 is measured when the effect of the compound reduces the luminescence signal by 50%.

In VivoGNF-6231 displays excellent pathway inhibition and induces robust antitumor efficacy in a mouse MMTV-WNT1 xenograft tumor model. GNF-6231 is moderately bound to mouse, rat, dog, monkey, and human plasma proteins (88.0, 83.1, 90.9, 71.2, and 95%, respectively). It shows good oral bioavailability, ranging from 72 to 96% in preclinical species (mouse, rat, and dog) when dosed in solution formulations. GNF-6231 is expected to have minimal to marginal distribution to tissues compared to total body water following intravenous administration to mouse (Vss 0.57 L/kg), rat (Vss 0.70 L/kg), and dog (Vss 0.25 L/kg).
Animal modelNude mice
Formulation & DosageDissolved in 20% (vol/vol) PEG300 and 30% (vol/vol) 10% ETPGS in water; 3 mg/kg; p.o.
References ACS Med Chem Lett. 2016 May 10;7(7):676-80.