CCT-251921
Based on 4 publication(s) in Google Scholar
CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.12%
- CAS 番号: 1607837-31-9
- 分子式: C21H23ClN6O
- 分子量:410.90
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 CCT-251921
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生物活性
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CDK8 2.3 nM (IC50) |
CDK19 2.6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COLO 205 | IC50 |
15 nM
Compound: 109
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Inhibition of WNT pathway activation in human COLO205 cells expressing APC mutant
Inhibition of WNT pathway activation in human COLO205 cells expressing APC mutant
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[PMID: 26796641] |
| LS174T | IC50 |
33 nM
Compound: 109
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Inhibition of WNT pathway activation in human LS174T cells expressing beta-catenin mutant
Inhibition of WNT pathway activation in human LS174T cells expressing beta-catenin mutant
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[PMID: 26796641] |
| MV4-11 | GI50 |
0.05 μM
Compound: CCT251921
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Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 72 hrs by resazurin assay
Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 72 hrs by resazurin assay
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[PMID: 33823391] |
| PA-1 | IC50 |
64 nM
Compound: 109
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Inhibition of WNT ligand dependent WNT pathway activation in human PA1 cells
Inhibition of WNT ligand dependent WNT pathway activation in human PA1 cells
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[PMID: 26796641] |
| SW480 | IC50 |
22 nM
Compound: 109
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Inhibition of WNT pathway activation in human SW480 cells expressing APC mutant
Inhibition of WNT pathway activation in human SW480 cells expressing APC mutant
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[PMID: 26796641] |
CCT-251921 has acceptable aqueous solubility and demonstrates minimal activity when tested in a panel of 55 receptors, ion channels, and enzymes at 1 μM and in a panel of 279 kinases; weak inhibition of CYPs is observed. CCT-251921 demonstrates potent inhibition of reporter-based readouts measuring basal WNT pathway activity in human cancer cell lines that have constitutively activated WNT pathway signaling: LS174T (β-catenin mutant), SW480 and Colo205 (APC mutant) or PA-1 human teratocarcinoma cells that are WNT ligand dependent[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1607837-31-9
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性状 Solid
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分子量 410.90
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分子式 C21H23ClN6O
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Color White to off-white
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SMILES
O=C1NCCC12CCN(C3=C(Cl)C(N)=NC=C3C4=CC5=C(N(C)N=C5)C=C4)CC2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Nucleic Acids Res
2021 Jul 21;49(13):7476-7491. PMID: 34197614 -
Pharmaceuticals (Basel)
New Assay Systems to Characterize the Broad-Spectrum Antiherpesviral and Non-Herpesviral Activity of Cyclin-Dependent Kinase (CDK) 8 Inhibitors. [Abstract]2025 Oct 16;18(10):1560. PMID: 41155676 -
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溶剤 & 溶解度
DMSO : 25 mg/mL (60.84 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (6.08 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 (6.08 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.
プロトコル
7dF3 cells are treated with CCT-251921 ranging in final concentration from 90 μM to 0.3 nM. After 2 h of further incubation, β-oestradiol is added to a final concentration of 10 μM. The cells are incubated and then 25 μL of luciferase reagent is added and mixed. After leaving the plate for 60 min at room temperature, luminescence is read on a plate luminescence reader[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Animals are dosed orally by gavage every 24 h at 0.1 mL per 10 g body weight. Tumors are measured three times weekly by Vernier calipers and body weights recorded. At the end of the study, animals are culled at intervals: 3 control and 3 treated at 1, 2, 6, and 24 h after the final dose. Heparinized blood is collected by cardiac puncture, spun, and plasma snap frozen for analysis of compound exposure. Tumors are excised, weighed and samples snap frozen for compound quantification and PD analyses. The 30 mg/kg q.d. schedule is well tolerated with no significant body weight loss. Tumor growth is significantly inhibited[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
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取扱説明書 (2659 KB)
参考文献
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4337 mL | 12.1684 mL | 24.3368 mL | 60.8421 mL |
| 5 mM | 0.4867 mL | 2.4337 mL | 4.8674 mL | 12.1684 mL | |
| 10 mM | 0.2434 mL | 1.2168 mL | 2.4337 mL | 6.0842 mL | |
| 15 mM | 0.1622 mL | 0.8112 mL | 1.6225 mL | 4.0561 mL | |
| 20 mM | 0.1217 mL | 0.6084 mL | 1.2168 mL | 3.0421 mL | |
| 25 mM | 0.0973 mL | 0.4867 mL | 0.9735 mL | 2.4337 mL | |
| 30 mM | 0.0811 mL | 0.4056 mL | 0.8112 mL | 2.0281 mL | |
| 40 mM | 0.0608 mL | 0.3042 mL | 0.6084 mL | 1.5211 mL | |
| 50 mM | 0.0487 mL | 0.2434 mL | 0.4867 mL | 1.2168 mL | |
| 60 mM | 0.0406 mL | 0.2028 mL | 0.4056 mL | 1.0140 mL |
CCT-251921 関連分類
HY-19984 関連分類
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