PROTAC CDK4/6 degrader 1
Based on 1 Customer Validation
PROTAC CDK4/6 degrader 1 is a CDK4/CDK6 PROTAC degrader, with DC50 values of 10.5 nM and 2.5 nM, respectively. PROTAC CDK4/6 degrader 1 inhibits the proliferation of Jurkat cells (IC50 = 0.18 μM), arrests the cell cycle at the G1 phase, and induces apoptosis. PROTAC CDK4/6 degrader 1 can be used for cancer research.
(Pink: CDK4 and CDK6 ligand (HY-163787); Blue: Cereblon ligand (HY-10984); Black: linker (HY-163788)).
For research use only. We do not sell to patients.
- Purity: 98.88%
- CAS No.: 3025082-14-5
- Formula: C41H47N11O6
- Molecular Weight:789.88
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Storage:
-20°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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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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CDK4 10.5 nM (DC50) |
CDK6 2.5 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
0.183 μM
Compound: 7f
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Anti-proliferative activity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Anti-proliferative activity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
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[PMID: 38943626] |
PROTAC CDK4/6 degrader 1 (Compound 7f) (72 h after initial 8 h pre-incubation) potently inhibits Jurkat cell proliferation with an IC50 of 0.183 μM[1].
PROTAC CDK4/6 degrader 1 (Compound 7f) (0.1-1 μM; 24 h) induces dose-dependent G1 phase cell cycle arrest in Jurkat cells by suppressing RB (Ser780) phosphorylation, reaching 50% G1 phase cells at 1 μM[1].
PROTAC CDK4/6 degrader 1 (Compound 7f) (0.1-2 μM; 24 h) induces dose-dependent apoptosis in Jurkat cells, with over 75% apoptotic cells at 2 μM[1].
PROTAC CDK4/6 degrader 1 (Compound 7f) (1-1000 nM) activates the Caspase-3 and PARP cleavage pathway in Jurkat cells in vitro in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat cells
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Concentration:0.1, 0.5 and 1 μM
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Incubation Time:24 h
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Result:Induced dose-dependent G1 phase cell cycle arrest in Jurkat cells, with the percentage of cells in G1 phase increasing from control levels to 50% at 1 μM.
Suppressed phosphorylation of RB (Ser780) at 1 μM, a key regulator of the G1-S cell cycle transition.
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Cell Line:Jurkat cells
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Concentration:0.1, 1 and 2 μM
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Incubation Time:24 h
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Result:Induced dose-dependent apoptosis in Jurkat cells, with the percentage of apoptotic cells increasing from control levels to over 75% at 2 μM.
Chemical Information
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CAS No. 3025082-14-5
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Appearance Solid
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Molecular Weight 789.88
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Formula C41H47N11O6
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Color Light yellow to orange
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SMILES
O=C1N(C2=NC(NC3=CC=C(C=C3)N4CCN(CC4)CCCCC(NCCNC5=CC=CC(C(N6C7CCC(NC7=O)=O)=O)=C5C6=O)=O)=NC=C2N=C1)C8CCCC8
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (126.60 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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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)
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 (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 | 1.2660 mL | 6.3301 mL | 12.6602 mL | 31.6504 mL |
| 5 mM | 0.2532 mL | 1.2660 mL | 2.5320 mL | 6.3301 mL | |
| 10 mM | 0.1266 mL | 0.6330 mL | 1.2660 mL | 3.1650 mL | |
| 15 mM | 0.0844 mL | 0.4220 mL | 0.8440 mL | 2.1100 mL | |
| 20 mM | 0.0633 mL | 0.3165 mL | 0.6330 mL | 1.5825 mL | |
| 25 mM | 0.0506 mL | 0.2532 mL | 0.5064 mL | 1.2660 mL | |
| 30 mM | 0.0422 mL | 0.2110 mL | 0.4220 mL | 1.0550 mL | |
| 40 mM | 0.0317 mL | 0.1583 mL | 0.3165 mL | 0.7913 mL | |
| 50 mM | 0.0253 mL | 0.1266 mL | 0.2532 mL | 0.6330 mL | |
| 60 mM | 0.0211 mL | 0.1055 mL | 0.2110 mL | 0.5275 mL | |
| 80 mM | 0.0158 mL | 0.0791 mL | 0.1583 mL | 0.3956 mL | |
| 100 mM | 0.0127 mL | 0.0633 mL | 0.1266 mL | 0.3165 mL |
PROTAC CDK4/6 degrader 1 Related Classifications
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