PROTAC CDK9 degrader-2
Based on 1 Customer Validation
PROTAC CDK9 degrader-2 is a PROTAC degrader targeting CDK9, with an IC50 of 523 nM. PROTAC CDK9 degrader-2 selectively degrades CDK9 via the cereblon-dependent ubiquitin-proteasome pathway and inhibits the proliferation of cancer cells overexpressing CDK9. PROTAC CDK9 degrader-2 can be used for cancer research.
(Pink: CDK9 ligand (HY-N0400); Blue: Cereblon ligand (HY-10984); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- 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
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
CDK9 523 nM (IC50) |
CDK9 17 μM (IC50, MCF-7 cells) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
17 μM
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Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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30196207 |
| L02 | IC50 |
> 100 μM
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Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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30196207 |
In Vitro
PROTAC CDK9 degrader-2 (compound 11c) (1-30 μM, 24 h) selectively induces concentration-dependent, proteasome-dependent, and CRBN-dependent degradation of CDK9 and its downstream Mcl-1 protein in MCF-7 cells[1].
PROTAC CDK9 degrader-2 (72 h) selectively inhibits the proliferation of MCF-7 cells with overexpressed CDK9, with an IC50 of 17 μM, while its activity against L02 cells with low CDK9 expression is negligible[1].
PROTAC CDK9 degrader-2 (10-20 μM; 24 h) induces dose-dependent apoptosis in MCF-7 cells following incubation at concentrations of 10 μM and 20 μM for 24 h[1].
PROTAC CDK9 degrader-2 (1 μM; 1 h) potently inhibits the kinase activity of recombinant CDK9/CycT1, with an IC50 value of 523 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:1, 10, 30 μM
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Incubation Time:24, 72 h
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Result:Induced concentration-dependent degradation of intracellular CDK9 protein, with no detectable effect on CDK2, CDK4, CDK5, CDK7, or CDK8 levels.
Caused concentration-dependent reduction of Mcl-1 protein levels.
Blocked Mcl-1 reduction when cells were pre-treated with MG132.
Reduced degradation of both CDK9 and Mcl-1 when cells were transfected with CRBN siRNA.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:10, 20 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner, with apoptotic cell populations increasing with higher concentrations of the compound.
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
In Vitro:
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)
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
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Data Sheet (280 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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