NCT02
Based on 1 Customer Validation
NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models.
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- Pureza: 98.14%
- No. CAS: 790245-61-3
- Fòrmula: C17H16N2O2S
- Peso molecular:312.39
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Actividad biológica
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Cereblon-DDB1 |
NCT02 (0-20 μM; 72 h) inhibits cell viability in colorectal cancer cell lines (TSC03, TSC08, TSC47, etc.) in a dose-dependent manner and has low toxicity to normal fibroblasts[1].
NCT02 (10 μM; 24-48 h) induces apoptosis in TSC03 and TSC14 cells, as evidenced by a significant increase in the proportion of lysed PARP-positive cells[1].
NCT02 (10 μM; 6 h) triggers the degradation of CCNK/CDK12 complex and significantly reduces CCNK protein levels, accompanied by a decrease in p-Ser2 POLR2 phosphorylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human colorectal cancer spheroids (TSC03, TSC08, TSC47, etc.), normal primary fibroblasts (HD-F)
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Concentration:0, 0.1, 1, 10, 20 μM
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Incubation Time:72 h
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Result:Significantly reduced viability of cancer cells in a dose-dependent manner, with IC50s ranging from 2.5-5.8 μM in sensitive TSCs (e.g., TSC03, TSC08).
Chemical Information
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No. CAS 790245-61-3
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Appearance Solid
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Peso molecular 312.39
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Fòrmula C17H16N2O2S
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Color Light yellow to light brown
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SMILES
O=C(NC1=NC=C(C)S1)CC2=COC3=CC4=C(CCC4)C=C32
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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 : 50 mg/mL (160.06 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 (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 3.2011 mL | 16.0056 mL | 32.0113 mL | 80.0282 mL |
| 5 mM | 0.6402 mL | 3.2011 mL | 6.4023 mL | 16.0056 mL | |
| 10 mM | 0.3201 mL | 1.6006 mL | 3.2011 mL | 8.0028 mL | |
| 15 mM | 0.2134 mL | 1.0670 mL | 2.1341 mL | 5.3352 mL | |
| 20 mM | 0.1601 mL | 0.8003 mL | 1.6006 mL | 4.0014 mL | |
| 25 mM | 0.1280 mL | 0.6402 mL | 1.2805 mL | 3.2011 mL | |
| 30 mM | 0.1067 mL | 0.5335 mL | 1.0670 mL | 2.6676 mL | |
| 40 mM | 0.0800 mL | 0.4001 mL | 0.8003 mL | 2.0007 mL | |
| 50 mM | 0.0640 mL | 0.3201 mL | 0.6402 mL | 1.6006 mL | |
| 60 mM | 0.0534 mL | 0.2668 mL | 0.5335 mL | 1.3338 mL | |
| 80 mM | 0.0400 mL | 0.2001 mL | 0.4001 mL | 1.0004 mL | |
| 100 mM | 0.0320 mL | 0.1601 mL | 0.3201 mL | 0.8003 mL |
NCT02 Related Classifications
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