PROTAC CDK2/4 Degrader-1
Based on 1 Customer Validation
PROTAC CDK2/4 Degrader-1 (Compound 5) is a CDK2/4 PROTAC degrader, with its DC50 values for CDK2 and CDK4 both ≤ 10 nM. PROTAC CDK2/4 Degrader-1 exhibits excellent inhibitory activity against cell proliferation in OVCAR3 and T47D cells. PROTAC CDK2/4 Degrader-1 can be used for research on breast cancer and ovarian cancer.
(Pink: CDK2 and CDK4 ligand (HY-W1047040); Blue: Cereblon ligand (HY-W883326); Black: linker).
For research use only. We do not sell to patients.
- Purity: 98.10%
- Formula: C30H39F2N9O5S
- Molecular Weight:675.75
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Storage: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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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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CDK2 ≤ 10 nM (DC50) |
CDK4 ≤ 10 nM (DC50) |
Cereblon |
Chemical Information
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Appearance Solid
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Molecular Weight 675.75
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Formula C30H39F2N9O5S
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Color White to off-white
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SMILES
O=S(NCCN(CC1)CCC1C(C=C2)=CC3=C2C(C(CC4)C(NC4=O)=O)=NN3C)(N5CCC(NC6=NC=C(OC(F)F)C=N6)CC5)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (147.98 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)
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 (3.70 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.70 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
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Data Sheet (275 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. 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 | 1.4798 mL | 7.3992 mL | 14.7984 mL | 36.9959 mL |
| 5 mM | 0.2960 mL | 1.4798 mL | 2.9597 mL | 7.3992 mL | |
| 10 mM | 0.1480 mL | 0.7399 mL | 1.4798 mL | 3.6996 mL | |
| 15 mM | 0.0987 mL | 0.4933 mL | 0.9866 mL | 2.4664 mL | |
| 20 mM | 0.0740 mL | 0.3700 mL | 0.7399 mL | 1.8498 mL | |
| 25 mM | 0.0592 mL | 0.2960 mL | 0.5919 mL | 1.4798 mL | |
| 30 mM | 0.0493 mL | 0.2466 mL | 0.4933 mL | 1.2332 mL | |
| 40 mM | 0.0370 mL | 0.1850 mL | 0.3700 mL | 0.9249 mL | |
| 50 mM | 0.0296 mL | 0.1480 mL | 0.2960 mL | 0.7399 mL | |
| 60 mM | 0.0247 mL | 0.1233 mL | 0.2466 mL | 0.6166 mL | |
| 80 mM | 0.0185 mL | 0.0925 mL | 0.1850 mL | 0.4624 mL | |
| 100 mM | 0.0148 mL | 0.0740 mL | 0.1480 mL | 0.3700 mL |
PROTAC CDK2/4 Degrader-1 Related Classifications
HY-179688 Related Classifications
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