PROTAC CDK2/9 Degrader-1
Based on 1 Customer Validation
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand.
(Pink: CDK2 and CDK9 ligand (HY-130980); Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 2408641-24-5
- Formula: C40H41N13O7
- Molecular Weight:815.84
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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 62 nM (DC50) |
CDK9 33 nM (DC50) |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
14.5 nM
Compound: F3
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Inhibition of tracer K10 binding to NanoLuc-CDK9/Cyclin T1 (unknown origin) expressed in human HEK293 cells after 1 hr in presence of ATP by NanoBRET assay
Inhibition of tracer K10 binding to NanoLuc-CDK9/Cyclin T1 (unknown origin) expressed in human HEK293 cells after 1 hr in presence of ATP by NanoBRET assay
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[PMID: 31846828] |
| HEK293 | IC50 |
7.42 nM
Compound: F3
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Inhibition of tracer K10 binding to NanoLuc-CDK2/Cyclin A (unknown origin) expressed in human HEK293 cells after 1 hr in presence of ATP by NanoBRET assay
Inhibition of tracer K10 binding to NanoLuc-CDK2/Cyclin A (unknown origin) expressed in human HEK293 cells after 1 hr in presence of ATP by NanoBRET assay
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[PMID: 31846828] |
| L02 | IC50 |
7.99 μM
Compound: F3
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Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 5 days by CCK-8 assay
Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 5 days by CCK-8 assay
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[PMID: 31846828] |
| PC-3 | DC50 |
33 nM
Compound: F3
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Protac activity at CRBN/CDK2/CDK9 in AR-negative human PC3 cells assessed as induction of CDK9 protein degradation after 24 hrs by Western blot analysis
Protac activity at CRBN/CDK2/CDK9 in AR-negative human PC3 cells assessed as induction of CDK9 protein degradation after 24 hrs by Western blot analysis
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[PMID: 31846828] |
| PC-3 | DC50 |
62 nM
Compound: F3
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Protac activity at CRBN/CDK2/CDK9 in AR-negative human PC3 cells assessed as induction of CDK2 protein degradation after 24 hrs by Western blot analysis
Protac activity at CRBN/CDK2/CDK9 in AR-negative human PC3 cells assessed as induction of CDK2 protein degradation after 24 hrs by Western blot analysis
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[PMID: 31846828] |
| PC-3 | IC50 |
0.12 μM
Compound: F3
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Antiproliferative activity against AR-negative human PC3 cells assessed as reduction in cell viability after 5 days by CCK8 assay
Antiproliferative activity against AR-negative human PC3 cells assessed as reduction in cell viability after 5 days by CCK8 assay
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[PMID: 31846828] |
PROTAC CDK2/9 Degrader-1 (0.25-3 μM; 48 hours) induces cell cycle blockage at the G2/M phase[1].
PROTAC CDK2/9 Degrader-1 (500 nM; 2-24 hours) down-regulates the Mcl-1 protein level in PC-3 cells[1].
PROTAC CDK2/9 Degrader-1 effectively degrades CDK2/9 in cell lines MCF-7, HCT-116 and 22Rv1, which all have high CDK2/9 expression[1].
PROTAC CDK2/9 Degrader-1 inhibits both CDK2 and CDK9, with IC50 as 7.42 nM and 14.50 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3 cells
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Concentration:500 nM
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Incubation Time:2, 4, 8, 16, 24 hours
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Result:Down-regulated the Mcl-1 protein level in PC-3 cells.
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Cell Line:PC-3 cells
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Concentration:0.25, 1, 3 μM
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Incubation Time:48 hours
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Result:Induced cell cycle blockage at the G2/M phase.
Chemical Information
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CAS No. 2408641-24-5
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Appearance Solid
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Molecular Weight 815.84
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Formula C40H41N13O7
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Color White to yellow
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SMILES
O=C(C1=NNC=C1NC2=C3C(NC=C3)=NC=N2)NC4=CC=C(CN5CCN(C(CCC(NCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)=O)CC5)C=C4
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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 : 50 mg/mL (61.29 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: 5 mg/mL (6.13 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Purity & Documentation
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Data Sheet (271 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 1.2257 mL | 6.1287 mL | 12.2573 mL | 30.6433 mL |
| 5 mM | 0.2451 mL | 1.2257 mL | 2.4515 mL | 6.1287 mL | |
| 10 mM | 0.1226 mL | 0.6129 mL | 1.2257 mL | 3.0643 mL | |
| 15 mM | 0.0817 mL | 0.4086 mL | 0.8172 mL | 2.0429 mL | |
| 20 mM | 0.0613 mL | 0.3064 mL | 0.6129 mL | 1.5322 mL | |
| 25 mM | 0.0490 mL | 0.2451 mL | 0.4903 mL | 1.2257 mL | |
| 30 mM | 0.0409 mL | 0.2043 mL | 0.4086 mL | 1.0214 mL | |
| 40 mM | 0.0306 mL | 0.1532 mL | 0.3064 mL | 0.7661 mL | |
| 50 mM | 0.0245 mL | 0.1226 mL | 0.2451 mL | 0.6129 mL | |
| 60 mM | 0.0204 mL | 0.1021 mL | 0.2043 mL | 0.5107 mL |
PROTAC CDK2/9 Degrader-1 Related Classifications
HY-130709 Related Classifications
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