GNF-6231

This product is for research use only, not for human use. We do not sell to patients.

GNF-6231
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
5mg$1353-6 Days
10mg$2103-6 Days
25mg$3603-6 Days
50mg$5403-6 Days
100mg$8153-6 Days
250mg$14003-6 Days
500mg$20203-6 Days

Cat #: V3197 CAS #: 1243244-74-7 Purity ≥ 98%

Description: GNF-6231 is a novel, potent, orally active and selective Porcupine inhibitor that blocks Wnt signaling with IC50 of 0.8 nM (Wnt3a Co-culture RGA). GNF-6231 has low/no drug drug interaction potential with IC50s of greater than 10 μM on all CYP isoforms tested. GNF-6231 showed excellent pathway inhibition and induced robust antitumor efficacy in a mouse MMTV-WNT1 xenograft tumor model. Targeting the aberrant Wnt signaling pathway is an attractive approach for the treatment of various cancers. Wnt signaling is tightly controlled during cellular proliferation, differentiation, and embryonic morphogenesis. Aberrant activation of this pathway plays a critical role in a variety of cancers including cutaneous squamous cell carcinoma (SCC), breast cancer, and colorectal cancer.

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Molecular Weight (MW)448.49
Molecular FormulaC24H25FN6O2
CAS No.1243244-74-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 90 mg/mL
Water: 5 mg/mL
Ethanol: < 1 mg/mL
SMILES CodeO=C(NC1=NC=C(N2CCN(C(C)=O)CC2)C=C1)CC3=CN=C(C4=CC(F)=NC=C4)C(C)=C3
SynonymsGNF6231; GNF 6231; GNF-6231
ProtocolIn VitroIn 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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.2297 mL11.1485 mL22.2970 mL44.5941 mL
5mM0.4459 mL2.2297 mL4.4594 mL8.9188 mL
10mM0.2230 mL1.1149 mL2.2297 mL4.4594 mL
20mM0.1115 mL0.5574 mL1.1149 mL2.2297 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.