PROTAC CDK9 degrader-2
Based on 1 Customer Validation
PROTAC CDK9 degrader-2 (compound 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines.
(Pink: CDK9 ligand (HY-N0400); Blue: Cereblon ligand (HY-10984); Black: linker).
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- Reinheit: 99.22%
- CAS. Nr.: 2435721-30-3
- Formel: C39H36N6O10
- Molecular Weight:748.74
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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CDK9 17 μM (IC50, MCF-7 cells) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L02 | IC50 |
>100 μM
Compound: 88
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Cytotoxicity against human L02 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
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[PMID: 32707525] |
| MCF7 | IC50 |
0.523 μM
Compound: 79
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Protac activity against E3 ubiquitin ligase/CDK9 in human MCF7 cells assessed as induction of CDK9 protein degradation
Protac activity against E3 ubiquitin ligase/CDK9 in human MCF7 cells assessed as induction of CDK9 protein degradation
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[PMID: 31035238] |
| MCF7 | IC50 |
17 nM
Compound: 45
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Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
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[PMID: 36205223] |
| MCF7 | IC50 |
17 μM
Compound: 15
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Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay
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[PMID: 31300317] |
| MCF7 | IC50 |
17 μM
Compound: 88
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay
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[PMID: 32707525] |
| MCF7 | IC50 |
17 μM
Compound: PROTAC 52
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Antiproliferative activity in human MCF7 cells assessed as cell growth inhibition
Antiproliferative activity in human MCF7 cells assessed as cell growth inhibition
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[PMID: 34411892] |
PROTAC CDK9 degrader-2 (IC50 = 17 μM, 72 h) inhibits proliferation of MCF-7 cells, and induces apoptosis, and is much less active against the CDK9 low-expressed L02 cells (IC50 > 100 μM)[1].
PROTAC CDK9 degrader-2 (1-30 μM, 24 h) selectively degrades CDK9 and Mcl-1 in a dose dependent manner in MCF-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2435721-30-3
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Appearance Solid
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Molecular Weight 748.74
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Formel C39H36N6O10
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Color Light yellow to yellow
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SMILES
O=C(C=C(C1=CC=CC=C1)O2)C3=C2C(OCC4=CN(CCCCCCCC(NC5=C(C(N(C6C(NC(CC6)=O)=O)C7=O)=O)C7=CC=C5)=O)N=N4)=C(O)C=C3O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (133.56 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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 (protect from light). 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 | 1.3356 mL | 6.6779 mL | 13.3558 mL | 33.3894 mL |
| 5 mM | 0.2671 mL | 1.3356 mL | 2.6712 mL | 6.6779 mL | |
| 10 mM | 0.1336 mL | 0.6678 mL | 1.3356 mL | 3.3389 mL | |
| 15 mM | 0.0890 mL | 0.4452 mL | 0.8904 mL | 2.2260 mL | |
| 20 mM | 0.0668 mL | 0.3339 mL | 0.6678 mL | 1.6695 mL | |
| 25 mM | 0.0534 mL | 0.2671 mL | 0.5342 mL | 1.3356 mL | |
| 30 mM | 0.0445 mL | 0.2226 mL | 0.4452 mL | 1.1130 mL | |
| 40 mM | 0.0334 mL | 0.1669 mL | 0.3339 mL | 0.8347 mL | |
| 50 mM | 0.0267 mL | 0.1336 mL | 0.2671 mL | 0.6678 mL | |
| 60 mM | 0.0223 mL | 0.1113 mL | 0.2226 mL | 0.5565 mL | |
| 80 mM | 0.0167 mL | 0.0835 mL | 0.1669 mL | 0.4174 mL | |
| 100 mM | 0.0134 mL | 0.0668 mL | 0.1336 mL | 0.3339 mL |
PROTAC CDK9 degrader-2 Related Classifications
HY-112811 Related Classifications
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