PP-C8
Based on 1 Customer Validation
PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC).
(Pink: CDK12/Cyclin K ligand (HY-176790); Blue: Cereblon ligand (HY-103597); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.99%
- No. CAS: 3032108-74-7
- Fòrmula: C43H51FN12O7
- Peso molecular:866.94
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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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CDK12/Cyclin K |
PP-C8 (0-30 μM; 24 hours; Bel-7402 and MDA-MB-231 cells) is a potent and highly selective CDK12-Cyclin K complex degrade[1].
PP-C8 (0-3 μM; 24 hours; Bel-7402 and MDA-MB-231 cells) mediated CDK12-CycK complex degradation is cereblon and UPS dependent PROTAC-MOA[1].
PP-C8 (0-3 μM; Bel-7402 and MDA-MB-231 cell lines) induces CDK12-Cyclin K degradation demonstrates superior synergistic antiproliferative activity with the PARP inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Bel-7402 and MDA-MB-231 cells
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Concentration:0, 0.1, 0.3 ,1.0, 3.0, 10.0 and 30.0 μM
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Incubation Time:24 hours
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Result:Downregulated of both CDK12 and CycK protein levels in a dose-dependent manner with DC50 of 416 nM and 412 nM.
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Cell Line:Bel-7402 and MDA-MB-231 cells
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Concentration:1 and 3 μM
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Incubation Time:24 hours
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Result:Nondegraded CDK12-CycK in neither CRBN nor neither UPS depleted cell lines.
Chemical Information
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No. CAS 3032108-74-7
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Appearance Solid
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Peso molecular 866.94
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Fòrmula C43H51FN12O7
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Color White to light yellow
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SMILES
CC(N1C=NC2=C1N=C(N=C2NCC3=NC4=CC(F)=C(C=C4N3)NCCCCCCCCNC(COC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)N8CCOCC8)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (115.35 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)
Pureza y Documentación
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Ficha de datos (270 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 | 1.1535 mL | 5.7674 mL | 11.5348 mL | 28.8371 mL |
| 5 mM | 0.2307 mL | 1.1535 mL | 2.3070 mL | 5.7674 mL | |
| 10 mM | 0.1153 mL | 0.5767 mL | 1.1535 mL | 2.8837 mL | |
| 15 mM | 0.0769 mL | 0.3845 mL | 0.7690 mL | 1.9225 mL | |
| 20 mM | 0.0577 mL | 0.2884 mL | 0.5767 mL | 1.4419 mL | |
| 25 mM | 0.0461 mL | 0.2307 mL | 0.4614 mL | 1.1535 mL | |
| 30 mM | 0.0384 mL | 0.1922 mL | 0.3845 mL | 0.9612 mL | |
| 40 mM | 0.0288 mL | 0.1442 mL | 0.2884 mL | 0.7209 mL | |
| 50 mM | 0.0231 mL | 0.1153 mL | 0.2307 mL | 0.5767 mL | |
| 60 mM | 0.0192 mL | 0.0961 mL | 0.1922 mL | 0.4806 mL | |
| 80 mM | 0.0144 mL | 0.0721 mL | 0.1442 mL | 0.3605 mL | |
| 100 mM | 0.0115 mL | 0.0577 mL | 0.1153 mL | 0.2884 mL |
PP-C8 Related Classifications
HY-144691 Related Classifications
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