GNF-6231

Name: GNF-6231
Brand: Selleck Chemicals
SKU: S8644
Rating: 5 (0 reviews)

For research use only.

Catalog No.S8644

CAS No. 1243245-18-2

GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.

Purity & Quality Control

Choose Selective PORCN Inhibitors

Biological Activity

Description

GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.

Targets

Porcupine ^[1]
(Cell-free)

0.8 nM

In vitro

GNF-6231 shows a good solubility. It 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^[1].

In vivo

GNF-6231 demonstrates 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)^[1].

Protocol

Cell Research:

^[1]

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Cell lines: TM3 Wnt-Luc cells and L-cell Wnt3A cells
Concentrations: --
Incubation Time: 24 h
Method:
The TM3 Wnt-Luc cells and L-cell Wnt3A cells are cocultured 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%. All compounds are tested in triplicates.

(Only for Reference)

Animal Research:

^[1]

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Animal Models: Nude mice
Dosages: 3 mg/kg
Administration: by oral gavage
(Only for Reference)

References

[1] Cheng D, et al. ACS Med Chem Lett. 2016, 7(7):676-80.

Solubility (25°C)

In vitro	DMSO	89 mg/mL (198.44 mM)
	Ethanol	5 mg/mL (11.14 mM)
	Water	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download GNF-6231 SDF

Molecular Weight	448.49
Formula	C₂₄H₂₅FN₆O₂
CAS No.	1243245-18-2
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC1=CC(=CN=C1C2=CC(=NC=C2)F)CC(=O)NC3=NC=C(C=C3)N4CCN(CC4)C(=O)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

Average weight of animals

g

Dosing volume per animal

ul

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Computed Result

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