PROTAC CDK9 degrader-4
Based on 1 Customer Validation
PROTAC CDK9 degrader-4 is a selective PROTAC CDK9 degrader. PROTAC CDK9 degrader-4 exhibits antiproliferative, pro-apoptotic and in vivo tumor growth inhibitory activities. PROTAC CDK9 degrader-4 can be used for the research of triple-negative breast cancer.
(Pink: CDK9 ligand (HY-115729); Blue: Cereblon ligand (HY-138793); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.65%
- CAS No.: 2411021-01-5
- Formula: C43H56N10O5
- Molecular Weight:792.97
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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CDK9 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-549 | IC50 |
13.6 μM
Compound: 45
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Growth inhibition of human BT-549 cells assessed as cell viability measured after 4 days by WST8 assay
Growth inhibition of human BT-549 cells assessed as cell viability measured after 4 days by WST8 assay
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[PMID: 34538051] |
| MDA-MB-231 | IC50 |
3.9 μM
Compound: 45
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Growth inhibition of human MDA-MB-231 cells assessed as cell viability measured after 4 days by WST8 assay
Growth inhibition of human MDA-MB-231 cells assessed as cell viability measured after 4 days by WST8 assay
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[PMID: 34538051] |
| MDA-MB-468 | IC50 |
15 μM
Compound: 45
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Growth inhibition of human MDA-MB-468 cells assessed as cell viability measured after 4 days by WST8 assay
Growth inhibition of human MDA-MB-468 cells assessed as cell viability measured after 4 days by WST8 assay
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[PMID: 34538051] |
PROTAC CDK9 degrader-4 (2.5-5.0 mg/kg; i.p.; once daily; 7 days) administered daily via intraperitoneal injection at 2.5 mg/kg and 5.0 mg/kg for 7 days significantly inhibits MDA-MB-231 TNBC tumor growth by selectively degrading CDK9, downregulating c-Myc, and reducing tumor cell proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice[1]
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Dosage:0.15 mM
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Administration:intratumoral injection; single dose
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Result:Decreased CDK9 protein levels by 54% compared to the vehicle-treated group.
Showed no significant change in CDK7 protein levels.
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Animal Model:Nude mice[1]
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Dosage:2.5 mg/kg; 5.0 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Inhibited tumor growth significantly over 7 days, with average endpoint tumor volume reduced by ~50% compared to the vehicle group.
Induced significant CDK9 degradation in tumor tissue at 2.5 mg/kg; induced stronger CDK9 degradation at 5.0 mg/kg, with no significant change in CDK7 protein levels for either dose.
Reduced CDK9-positive cells by 62.3% at 2.5 mg/kg, and by 90.8% at 5.0 mg/kg.
Reduced c-Myc-positive cells by 41.0% at 2.5 mg/kg, and by 76.7% at 5.0 mg/kg.
Reduced Ki67-positive cells by 32.8% at 2.5 mg/kg, and by 69.7% at 5.0 mg/kg.
Showed no significant change in CDK7-positive cells at 2.5 mg/kg; reduced CDK7-positive cells by 12.4% at 5.0 mg/kg.
Caused slight body weight loss on day 7 compared to the vehicle group.
Chemical Information
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CAS No. 2411021-01-5
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Appearance Solid
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Molecular Weight 792.97
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Formula C43H56N10O5
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Color White to yellow
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SMILES
O=C(N1CCN(CCCCCC2=CC=CC3=C2CN(C(CC4)C(NC4=O)=O)C3=O)CC1)NC5=CC=C(CNC6=CC(N[C@H](CO)CC)=NC7=C(C(C)C)C=NN67)C=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (126.11 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)
Purity & Documentation
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Data Sheet (271 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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Handling Instructions (2659 KB)
References
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 | 1.2611 mL | 6.3054 mL | 12.6108 mL | 31.5270 mL |
| 5 mM | 0.2522 mL | 1.2611 mL | 2.5222 mL | 6.3054 mL | |
| 10 mM | 0.1261 mL | 0.6305 mL | 1.2611 mL | 3.1527 mL | |
| 15 mM | 0.0841 mL | 0.4204 mL | 0.8407 mL | 2.1018 mL | |
| 20 mM | 0.0631 mL | 0.3153 mL | 0.6305 mL | 1.5764 mL | |
| 25 mM | 0.0504 mL | 0.2522 mL | 0.5044 mL | 1.2611 mL | |
| 30 mM | 0.0420 mL | 0.2102 mL | 0.4204 mL | 1.0509 mL | |
| 40 mM | 0.0315 mL | 0.1576 mL | 0.3153 mL | 0.7882 mL | |
| 50 mM | 0.0252 mL | 0.1261 mL | 0.2522 mL | 0.6305 mL | |
| 60 mM | 0.0210 mL | 0.1051 mL | 0.2102 mL | 0.5255 mL | |
| 80 mM | 0.0158 mL | 0.0788 mL | 0.1576 mL | 0.3941 mL | |
| 100 mM | 0.0126 mL | 0.0631 mL | 0.1261 mL | 0.3153 mL |
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