G-631
Based on 1 Customer Validation
G-631 is an orally active tankyrase(TNKS1/TNKS2) inhibitor. G-631 stabilizes AXIN and inhibits the Wnt/β-catenin signaling pathway. G-631 can be used in studies related to cancers such as colorectal cancer.
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 1507370-78-6
- Formula: C19H22F2N6O3
- Molecular Weight:420.41
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
G-631 is a potent and selective TNKS1/2 inhibitor, with a biochemical IC50 of 7 nM and a cellular IC50 of 8 nM in HEK293 cells[1].
G-631 (10 μM) exhibits 56% binding inhibitory activity against the human norepinephrine transporter[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-24 | Cmax | Tmax | AUC |
|---|---|---|---|---|---|---|
| Mice[1] | 6.5 mg/kg | p.o. | 25.7 μM·h | 7.81 μM | 0.5 h | 1.66 |
| Mice[1] | 12.5 mg/kg | p.o. | 54.1 μM·h | 11.7 μM | 0.5 h | 1.82 |
| Mice[1] | 25 mg/kg | p.o. | 52.8 μM·h | 21.4 μM | 0.5 h | 0.887 |
| Mice[1] | 50 mg/kg | p.o. | 83.2 μM·h | 20.7 μM | 0.5 h | 0.699 |
| Mice[1] | 100 mg/kg | p.o. | 114 μM·h | 40.3 μM | 0.5 h | 0.479 |
| Mice[1] | 25 mg/kg | p.o. | / | 7.4 μM | 1.0 h | / |
| Mice[1] | 25 mg/kg | p.o. | / | 6.8 μM | 1.0 h | / |
| Mice[1] | 100 mg/kg | p.o. | / | 23.4 μM | 1.0 h | / |
| Mice[1] | 100 mg/kg | p.o. | / | 13.9 μM | 1.0 h | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nu/nu mice (female, 6-8 weeks of age, implanted with SW403 colorectal adenocarcinoma cells)[1]
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Dosage:6.25-100 mg/kg; 25 mg/kg (twice daily, not tolerated); 50 mg/kg (twice daily, not tolerated); 100 mg/kg (once daily, MTD)
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Administration:p.o.; once daily; 21 days; p.o.; twice daily; 21 days
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Result:Caused a dose-dependent reduction in relative TNFRSF19 mRNA levels in tumors.
Reduced mean tumor volume.
Induced approximately 10% body weight loss at 100 mg/kg once daily.
Was not tolerated at 25 and 50 mg/kg twice daily, with greater than 10% body weight loss.
Chemical Information
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CAS No. 1507370-78-6
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Appearance Solid
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Molecular Weight 420.41
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Formula C19H22F2N6O3
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Color White to off-white
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SMILES
O=C1N=C(N2CCN(CC2)C3=C(C=C(C=C3F)OCCOC)F)NC4=C1C=NN4C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 2 mg/mL (4.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3786 mL | 11.8932 mL | 23.7863 mL | 59.4658 mL |
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