PROTAC CDK9 degrader-9
Based on 1 Customer Validation
PROTAC CDK9 degrader-9 is an orally active, selective CDK9 PROTAC degrader with a DC50 of 3.94 nM. PROTAC CDK9 degrader-9 downregulates downstream targets c-Myc and MCL-1. PROTAC CDK9 degrader-9 inhibits the proliferation of breast cancer cells. PROTAC CDK9 degrader-9 can be used for the research of triple-negative breast cancer.
(Pink: CDK9 ligand (HY-182810); Blue: Cereblon ligand (HY-W998346); Black: linker).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.25%
- CAS No.: 3117192-80-7
- Formule: C42H51FN12O6
- Masse moléculaire:838.93
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Stockage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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CDK9 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:0.01, 0.1, 0.5, and 2.5 μM
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Incubation Time:4 h, 8 h
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Result:Did not affect protein levels of CDK1, CDK2, CDK4, CDK5, CDK6, or CDK7 at concentrations ranging from 0.01 μM to 2.5 μM.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft with MDA-MB-231 cells)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:p.o.; daily; 12 days
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Result:Achieved 60.5% tumor growth inhibition compared to vehicle at 10 mg/kg dose.
Induced slight, non-significant body weight loss at 10 mg/kg dose.
Marked CDK9 protein depletion in tumor tissue at 10 mg/kg dose.
Substantially reduced c-Myc and MCL-1 protein levels in tumor tissue at 10 mg/kg dose.
Slightly increased cleaved caspase-3 (apoptosis marker) in tumor tissue detected by immunohistochemistry at 10 mg/kg dose.
Showed no significant anti-tumor effects at 5 mg/kg dose.
Showed no CDK9 depletion in tumor tissue at 5 mg/kg dose.
Chemical Information
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CAS No. 3117192-80-7
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Appearance Solid
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Masse moléculaire 838.93
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Formule C42H51FN12O6
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Color Off-white to light yellow
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SMILES
O=C1N(C2CCC(NC2=O)=O)C(C3=C1C=C(F)C(N(CC4)CCN4C5CCN(C(NC6=CC=C(CNC7=NC(N[C@H](CO)CC)=NC8=C(C(C)C)C=NN87)C=C6)=O)CC5)=C3)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (59.60 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 (protect from light, stored under nitrogen). 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, stored under nitrogen). 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.98 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 (2.98 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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 (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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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 (protect from light, stored under nitrogen). 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 | 1.1920 mL | 5.9600 mL | 11.9199 mL | 29.7999 mL |
| 5 mM | 0.2384 mL | 1.1920 mL | 2.3840 mL | 5.9600 mL | |
| 10 mM | 0.1192 mL | 0.5960 mL | 1.1920 mL | 2.9800 mL | |
| 15 mM | 0.0795 mL | 0.3973 mL | 0.7947 mL | 1.9867 mL | |
| 20 mM | 0.0596 mL | 0.2980 mL | 0.5960 mL | 1.4900 mL | |
| 25 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 1.1920 mL | |
| 30 mM | 0.0397 mL | 0.1987 mL | 0.3973 mL | 0.9933 mL | |
| 40 mM | 0.0298 mL | 0.1490 mL | 0.2980 mL | 0.7450 mL | |
| 50 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5960 mL |
PROTAC CDK9 degrader-9 Related Classifications
HY-168518 Related Classifications
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