CRT0066854
Based on 1 Customer Validation
CRT0066854 is a potent and selective atypical PKC isoenzymes inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively.
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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: 98.85%
- CAS 番号: 1438881-19-6
- 分子式: C24H25N5S
- 分子量:415.55
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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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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PKCζ 639 nM (IC50) |
ROCK2 620 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Huh-7 | GI50 |
3.1 μM
Compound: CRT0066854
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Antiproliferative activity against human HuH7 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human HuH7 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 30891133] |
CRT0066854 displaces a crucial Asn-Phe-Asp motif that is part of the adenosine-binding pocket and engages an acidic patch used by arginine-rich PKC substrates[1].CRT0066854 (0.2-1.2 μM; 6 days) is able to restore polarized morphogenesis in the dysplastic H-Ras spheroids, and the maximal proportion of spheroids with PSALs is at the lower dose of 1.2 μM[1].
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 1438881-19-6
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性状 Solid
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分子量 415.55
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分子式 C24H25N5S
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Color White to yellow
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SMILES
N[C@H](CNC1=NC(C2=CC=NC=C2)=NC3=C1C(CCCC4)=C4S3)CC5=CC=CC=C5
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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
溶剤 & 溶解度
DMSO : 50 mg/mL (120.32 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, 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 (6.02 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 (6.02 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.
純度とドキュメンテーション
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データシート (278 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 | 2.4064 mL | 12.0322 mL | 24.0645 mL | 60.1612 mL |
| 5 mM | 0.4813 mL | 2.4064 mL | 4.8129 mL | 12.0322 mL | |
| 10 mM | 0.2406 mL | 1.2032 mL | 2.4064 mL | 6.0161 mL | |
| 15 mM | 0.1604 mL | 0.8021 mL | 1.6043 mL | 4.0107 mL | |
| 20 mM | 0.1203 mL | 0.6016 mL | 1.2032 mL | 3.0081 mL | |
| 25 mM | 0.0963 mL | 0.4813 mL | 0.9626 mL | 2.4064 mL | |
| 30 mM | 0.0802 mL | 0.4011 mL | 0.8021 mL | 2.0054 mL | |
| 40 mM | 0.0602 mL | 0.3008 mL | 0.6016 mL | 1.5040 mL | |
| 50 mM | 0.0481 mL | 0.2406 mL | 0.4813 mL | 1.2032 mL | |
| 60 mM | 0.0401 mL | 0.2005 mL | 0.4011 mL | 1.0027 mL | |
| 80 mM | 0.0301 mL | 0.1504 mL | 0.3008 mL | 0.7520 mL | |
| 100 mM | 0.0241 mL | 0.1203 mL | 0.2406 mL | 0.6016 mL |
CRT0066854 関連分類
HY-18713 関連分類
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