dCDK9-202
Based on 1 Customer Validation
dCDK9-202 a potent CDK9 PROTAC degrader with an DC50 value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015)).
(Pink: CDK9 ligand (HY-10008); Blue: Cereblon ligand (HY-W248665); Black: linker (HY-N8015)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.74%
- Formule: C40H49N7O7S2
- Masse moléculaire:803.99
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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
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Activité biologique
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CDK9 3.5 nM (DC50) |
Caspase-3 |
Caspase-7 |
Cereblon |
dCDK9-202 (10 nM, 0-24 h) treatment of TC-71 cells within 2 hours can significantly reduce the CDK9 protein level, and complete and nearly continuous degradation was achieved within 8 hours[1].
dCDK9-202 (0.1 nM-1 μM, 24 h) exhibitx nanomolar levels of proliferation inhibitory activity in 12 cancer cell lines derived from various tissues such as lung, liver, bone, and brain. For instance, in TC-71 cells, the IC₅₀ is 8.5 nM[1].
dCDK9-202 (10-50 nM, 24 h) activates Caspase-3/7, increases the level of cleaved PARP, and directly induces apoptosis of TC-71 cells[1].
dCDK9-202 (0.25-25 nM, 6 h) significantly reduces the phosphorylation of Ser2 in the CTD domain of RNA polymerase II (p-Rpb1 Ser2) and downregulates a variety of short half-life proteins that are regulated by CDK9 and are closely related to cancer occurrence in TC-71 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TC-71 cells
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Concentration:10 and 50 nM
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Incubation Time:24 h
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Result:Activated Caspase-3/7, increased the level of cleaved PARP.
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Cell Line:TC-71 cells
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Concentration:0.25, 2.5 and 25 nM
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Incubation Time:6 h
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Result:Significantly reduced the phosphorylation of Ser2 in the CTD domain of RNA polymerase II (p-Rpb1 Ser2).
Strongly down-regulated a variety of short half-life proteins that are regulated by CDK9 and are closely related to cancer occurrence, such as MYC, MCL1, BCL-xL, etc.
| Species | Dose | Route | T1/2 | Cmax | AUC0-t | CL | Vss |
|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 0.3 h | 280 ng/mL | 116 ng·h/mL | 312 mL/min/kg | 7.1 L/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:TC-71 cells xenografts model established in NCG mice (female, 6-8 weeks)[1]
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Dosage:10 mg/kg
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Administration:Intravenous injection (i.v.), once every other days for 7 doses
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Result:Significantly inhibited the tumor volume and weight.
Effectively reduced the level of CDK9 protein in tumor tissues after a single administration 2 hours later.
Did not show any weight loss or other obvious signs of toxicity in mice.
Chemical Information
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Appearance Solid
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Masse moléculaire 803.99
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Formule C40H49N7O7S2
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Color White to off-white
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SMILES
CC(C)(C1=CN=C(O1)CSC2=CN=C(S2)NC(C3CCN(CC3)C(CCCCCCCN4CC5=C(C4)C=C6C(N(C(C6=C5)=O)C7CCC(NC7=O)=O)=O)=O)=O)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 : 100 mg/mL (124.38 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 (3.11 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 (3.11 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.
Pureté et documentation
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Fiche technique (273 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. 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 | 1.2438 mL | 6.2190 mL | 12.4380 mL | 31.0949 mL |
| 5 mM | 0.2488 mL | 1.2438 mL | 2.4876 mL | 6.2190 mL | |
| 10 mM | 0.1244 mL | 0.6219 mL | 1.2438 mL | 3.1095 mL | |
| 15 mM | 0.0829 mL | 0.4146 mL | 0.8292 mL | 2.0730 mL | |
| 20 mM | 0.0622 mL | 0.3109 mL | 0.6219 mL | 1.5547 mL | |
| 25 mM | 0.0498 mL | 0.2488 mL | 0.4975 mL | 1.2438 mL | |
| 30 mM | 0.0415 mL | 0.2073 mL | 0.4146 mL | 1.0365 mL | |
| 40 mM | 0.0311 mL | 0.1555 mL | 0.3109 mL | 0.7774 mL | |
| 50 mM | 0.0249 mL | 0.1244 mL | 0.2488 mL | 0.6219 mL | |
| 60 mM | 0.0207 mL | 0.1036 mL | 0.2073 mL | 0.5182 mL | |
| 80 mM | 0.0155 mL | 0.0777 mL | 0.1555 mL | 0.3887 mL | |
| 100 mM | 0.0124 mL | 0.0622 mL | 0.1244 mL | 0.3109 mL |
dCDK9-202 Related Classifications
HY-178861 Related Classifications
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