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).
For research use only. We do not sell to patients.
- Purity: 99.99%
- CAS No.: 3032108-74-7
- Formula: C43H51FN12O7
- Molecular Weight:866.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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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
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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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CAS No. 3032108-74-7
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Appearance Solid
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Molecular Weight 866.94
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
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)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (270 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
| 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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