PROTAC CDK9 degrader-7
Based on 1 Customer Validation
PROTAC CDK9 degrader-7 is a CDK9 PROTAC degrader that mediates CDK9 degradation through the proteasome. PROTAC CDK9 degrader-7 reduces MCL-1 levels and exhibits antiproliferative activity in leukemia cells. PROTAC CDK9 degrader-7 can be used for research on acute myeloid leukemia.
(Pink: CDK9/Cyclin T ligand (HY-50940); Blue: Cereblon ligand (HY-103597); Black: linker).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.62%
- CAS No.: 2935587-90-7
- Formule: C43H50Cl2N8O9
- Masse moléculaire:893.81
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
Description
IC50 & Target
[1]|
CDK9 |
MCL1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
0.04 μM
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Antiproliferative activity against human Molm-13 AML cells assessed as viability reduction by MTS assay.
Antiproliferative activity against human Molm-13 AML cells assessed as viability reduction by MTS assay.
|
37071962 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 AML cells
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Concentration:0.01, 0.05, 0.1, 0.5, 1, and 5 μM; 1 μM (comparative blot)
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Incubation Time:6 h
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Result:Produced significant CDK9 degradation and reduced MCL-1 levels at 1 μM.
Showed among the most potent activity in the aminoalkanoic acid series.
CDK9 and MCL1 signals decreased with increasing concentration across 0.01-5 μM after 6 h.
BCL2 was also probed.
Chemical Information
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CAS No. 2935587-90-7
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Appearance Solid
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Masse moléculaire 893.81
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Formule C43H50Cl2N8O9
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Color White to off-white
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SMILES
O=C(NCCCCCCCCCCCC(N1CCC(CC1)NC(C2=NNC=C2NC(C3=C(C=CC=C3Cl)Cl)=O)=O)=O)COC4=CC=CC5=C4C(N(C5=O)C6CCC(NC6=O)=O)=O
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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
In Vitro:
DMSO : 100 mg/mL (111.88 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)
In Vivo:
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.
In Vivo Dissolution Calculator
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 (272 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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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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1188 mL | 5.5940 mL | 11.1881 mL | 27.9702 mL |
| 5 mM | 0.2238 mL | 1.1188 mL | 2.2376 mL | 5.5940 mL | |
| 10 mM | 0.1119 mL | 0.5594 mL | 1.1188 mL | 2.7970 mL | |
| 15 mM | 0.0746 mL | 0.3729 mL | 0.7459 mL | 1.8647 mL | |
| 20 mM | 0.0559 mL | 0.2797 mL | 0.5594 mL | 1.3985 mL | |
| 25 mM | 0.0448 mL | 0.2238 mL | 0.4475 mL | 1.1188 mL | |
| 30 mM | 0.0373 mL | 0.1865 mL | 0.3729 mL | 0.9323 mL | |
| 40 mM | 0.0280 mL | 0.1399 mL | 0.2797 mL | 0.6993 mL | |
| 50 mM | 0.0224 mL | 0.1119 mL | 0.2238 mL | 0.5594 mL | |
| 60 mM | 0.0186 mL | 0.0932 mL | 0.1865 mL | 0.4662 mL | |
| 80 mM | 0.0140 mL | 0.0699 mL | 0.1399 mL | 0.3496 mL | |
| 100 mM | 0.0112 mL | 0.0559 mL | 0.1119 mL | 0.2797 mL |