CDK4 degrader 1
Based on 1 Customer Validation
CDK4 degrader 1 is a selective CDK4 molecular glue degrader. CDK4 degrader 1 induces intracellular CDK4 degradation, and its activity is dependent on DCAF16. CDK4 degrader 1 targets the cysteine residue on DCAF16 through its vinylsulfonylpiperazine domain, thereby mediating the degradation of CDK4. CDK4 degrader 1 can be used in research related to cervical cancer.
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- Pureté: 99.83%
- CAS No.: 3094209-58-9
- Formule: C25H32N8O3S
- Masse moléculaire:524.64
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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CDK4 |
DCAF16 |
CDK4 degrader 1 (mL 1-71) (0.1-10 μM; 24 h) induces dose-dependent degradation of CDK4 in C33A cervical cancer cells, with the most significant effect observed after treatment with 10 μM for 24 h[1].
Treatment of C33A cervical cancer cells with CDK4 degrader 1 (10 μM; 24 h) for 24 h at 10 μM induces relatively selective degradation of CDK4[1].
CDK4 degrader 1 (0.1-10 μM; 24 h) induces dose-dependent degradation of CDK4 in DCAF16 wild-type HEK293 cells, while this effect is significantly attenuated in DCAF16 knockout HEK293 cells, indicating that its activity is dependent on DCAF16[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C33A cervical cancer cells
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Concentration:0.1 μM; 1 μM; 5 μM; 10 μM
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Incubation Time:24 h
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Result:Induced dose-dependent degradation of CDK4.
Reduced CDK4 levels to approximately 0.25 relative to control at 10 μM.
Produced progressively smaller reductions at lower concentrations.
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Cell Line:DCAF16 wild-type (WT) and knockout (KO) HEK293 cells
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Concentration:0.1 μM; 1 μM; 5 μM; 10 μM
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Incubation Time:24 h
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Result:Induced dose-dependent degradation of CDK4 in DCAF16 WT HEK293 cells.
Reduced CDK4 levels to approximately 0.3 relative to control at 10 μM in DCAF16 WT HEK293 cells.
Significantly attenuated degradation of CDK4 across all tested concentrations in DCAF16 KO HEK293 cells.
Chemical Information
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CAS No. 3094209-58-9
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Appearance Solid
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Masse moléculaire 524.64
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Formule C25H32N8O3S
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Color White to off-white
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SMILES
O=C(C1=CC2=CN=C(NC3=NC=C(N4CCN(S(=O)(C=C)=O)CC4)C=C3)N=C2N1C5CCCC5)N(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 25 mg/mL (47.65 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)
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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (273 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 1.9061 mL | 9.5303 mL | 19.0607 mL | 47.6517 mL |
| 5 mM | 0.3812 mL | 1.9061 mL | 3.8121 mL | 9.5303 mL | |
| 10 mM | 0.1906 mL | 0.9530 mL | 1.9061 mL | 4.7652 mL | |
| 15 mM | 0.1271 mL | 0.6354 mL | 1.2707 mL | 3.1768 mL | |
| 20 mM | 0.0953 mL | 0.4765 mL | 0.9530 mL | 2.3826 mL | |
| 25 mM | 0.0762 mL | 0.3812 mL | 0.7624 mL | 1.9061 mL | |
| 30 mM | 0.0635 mL | 0.3177 mL | 0.6354 mL | 1.5884 mL | |
| 40 mM | 0.0477 mL | 0.2383 mL | 0.4765 mL | 1.1913 mL |
CDK4 degrader 1 Related Classifications
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