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| Size | Price | Stock |
|---|---|---|
| 5mg | $135 | 3-6 Days |
| 10mg | $210 | 3-6 Days |
| 25mg | $360 | 3-6 Days |
| 50mg | $540 | 3-6 Days |
| 100mg | $815 | 3-6 Days |
| 250mg | $1400 | 3-6 Days |
| 500mg | $2020 | 3-6 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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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 448.49 |
|---|---|
| Molecular Formula | C24H25FN6O2 |
| CAS No. | 1243244-74-7 |
| 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 | |
| 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 |
| Synonyms | GNF6231; GNF 6231; GNF-6231 |
| Protocol | 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 Vivo | GNF-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 model | Nude mice |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.2297 mL | 11.1485 mL | 22.2970 mL | 44.5941 mL |
| 5mM | 0.4459 mL | 2.2297 mL | 4.4594 mL | 8.9188 mL |
| 10mM | 0.2230 mL | 1.1149 mL | 2.2297 mL | 4.4594 mL |
| 20mM | 0.1115 mL | 0.5574 mL | 1.1149 mL | 2.2297 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.