MSC2504877
Based on 1 Customer Validation
MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC50s of 0.0007, 0.0008, 0.54 µM for TNKS, TNKS2, PARP1, respectively. MSC2504877 increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels. MSC2504877 shows anti-tumor activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.25%
- No. CAS: 1460286-21-8
- Fòrmula: C17H18N2O2
- Peso molecular:282.34
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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PARP1 0.54 μM (IC50) |
TNKS 0.0007 μM (IC50) |
TNKS2 0.0008 μM (IC50) |
MSC2504877 (1, 3, 10 µM; 24 h) increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels in APC mutant COLO320DM colorectal tumor cells[1].
MSC2504877 (0-100 µM; 5 days) inhibits the survival of APC−/− cells and COLO320DM cells[1].
MSC2504877 (1 µM; 24 h) combinant with albociclib (HY-50767) (0.03 µM) induces cell cycle arrest at G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:APC mutant COLO320DM colorectal tumour cells
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Concentration:1, 3, 10 µM
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Incubation Time:24 h
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Result:Increased AXIN2 protein levels and decreased β-catenin levels.
MSC2504877 (30 mg/kg+ palbociclib (HY-50767) 150 mg/kg; p.o.; once) suppresses hyperproliferation in Apc defective cells in vivo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17 SCID mice (APC mutant COLO320DM tumour cell xenografts)[1]
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Dosage:30 mg/kg
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Administration:P.o.; once
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Result:Elicited an increase in both TNKS and AXIN2 levels in tumours, peaking at 6–10 hours after drug administration and falling 18 hours after.
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Animal Model:Villin-CreERT2; Apcfl/fl mice[1]
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Dosage:50 mg/kg + palbociclib (150 mg/kg)
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Administration:P.o.; once
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Result:Suppressed the expression of the archetypal Wnt target gene and stem cell marker Lgr5 and combination drug treatment caused a profound increase in nuclear p21.
Chemical Information
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No. CAS 1460286-21-8
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Appearance Solid
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Peso molecular 282.34
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Fòrmula C17H18N2O2
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Color Off-white to light yellow
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SMILES
O=C1C2=CC=C(C)N2C=C(C3=CC=C(C(C)(O)C)C=C3)N1
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Synonyms
M2912
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 125 mg/mL (442.73 mM; Need ultrasonic; 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)
Pureza y Documentación
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Ficha de datos (275 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 3.5418 mL | 17.7091 mL | 35.4183 mL | 88.5457 mL |
| 5 mM | 0.7084 mL | 3.5418 mL | 7.0837 mL | 17.7091 mL | |
| 10 mM | 0.3542 mL | 1.7709 mL | 3.5418 mL | 8.8546 mL | |
| 15 mM | 0.2361 mL | 1.1806 mL | 2.3612 mL | 5.9030 mL | |
| 20 mM | 0.1771 mL | 0.8855 mL | 1.7709 mL | 4.4273 mL | |
| 25 mM | 0.1417 mL | 0.7084 mL | 1.4167 mL | 3.5418 mL | |
| 30 mM | 0.1181 mL | 0.5903 mL | 1.1806 mL | 2.9515 mL | |
| 40 mM | 0.0885 mL | 0.4427 mL | 0.8855 mL | 2.2136 mL | |
| 50 mM | 0.0708 mL | 0.3542 mL | 0.7084 mL | 1.7709 mL | |
| 60 mM | 0.0590 mL | 0.2952 mL | 0.5903 mL | 1.4758 mL | |
| 80 mM | 0.0443 mL | 0.2214 mL | 0.4427 mL | 1.1068 mL | |
| 100 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.8855 mL |
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