NU6027
Based on 1 Customer Validation
NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 μM and 1.3 μM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.
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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 : 98.01%
- CAS 番号: 220036-08-8
- 分子式: C11H17N5O2
- 分子量:251.28
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
- 参考文献
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Help & FAQs
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Aminopurvalanol ACyclins/Cdk Inhibitor
生物活性
製品説明
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CDK1 2.5 μM (Ki) |
CDK2 1.3 μM (Ki) |
ATR |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MCF7 | IC50 |
6.7 μM
Compound: 46, NU6027
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Inhibition of ATR autophosphorylation in irradiated human MCF7 cells compound treated for 2 hr before and 1 hr after irradiation by Western blot method
Inhibition of ATR autophosphorylation in irradiated human MCF7 cells compound treated for 2 hr before and 1 hr after irradiation by Western blot method
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[PMID: 22835870] |
| Oocyte | IC50 |
2.9 μM
Compound: 1a
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Inhibition of Cyclin dependent kinase 1-cyclin B1 from starfish oocytes at 12.5 uM ATP
Inhibition of Cyclin dependent kinase 1-cyclin B1 from starfish oocytes at 12.5 uM ATP
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[PMID: 12482427] |
| Sf9 | IC50 |
2.2 μM
Compound: NU6027
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Inhibition of human CDK2/Cyclin A expressed in baculovirus infected Sf9 insect cells
Inhibition of human CDK2/Cyclin A expressed in baculovirus infected Sf9 insect cells
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[PMID: 30543440] |
体外実験
NU6027 (1 nM-100 μM; 48 h) inhibits the growth of human tumor cells with a GI50 of 10±6 μM[1].
NU6027 (0.1-25 μM; 24 h) inhibits ATR activity with an IC50 of 2.8 μM in GM847KD cells. NU6027 (1-10 μM; 24 h) inhibits ATR activity with an IC50 of 6.7±2.3 μM in MCF7 cells[2].
NU6027 (4 or 10 μM; 24 h) attenuates G2/M arrest following DNA damage in MCF7 cells[2].
NU6027 (10 μM; 24 h) significantly reduces RAD51 foci in both control and PF-01367338-treated V-C8 B2 cells[2].
NU6027 (4 μM; 24 h) causes 82% suppression of the increase in RAD51 foci-positive cells treated by PF-01367338[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MCF7 cells
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Concentration:0, 1, 5, 10 μM
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Incubation Time:24 h
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Result:Inhibited CDK2-mediated pRbT821 by 42±27% compared with 70±12% inhibition of pCHK1S345 with the concentration of 10 µM.
化学情報
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CAS 番号 220036-08-8
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性状 Solid
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分子量 251.28
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分子式 C11H17N5O2
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Color Pale purple to purple
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SMILES
NC1=NC(OCC2CCCCC2)=C(N=O)C(N)=N1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
DMSO : 12.5 mg/mL (49.75 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). 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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: ≥ 1.25 mg/mL (4.97 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (4.97 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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)
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
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Arris CE, et, al. Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J Med Chem. 2000 Jul 27; 43(15): 2797-804. [Content Brief]
[2]. Peasland A, et, al. Identification and evaluation of a potent novel ATR inhibitor, NU6027, in breast and ovarian cancer cell lines. Br J Cancer. 2011 Jul 26;105(3):372-81. [Content Brief]
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). 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 | 3.9796 mL | 19.8981 mL | 39.7962 mL | 99.4906 mL |
| 5 mM | 0.7959 mL | 3.9796 mL | 7.9592 mL | 19.8981 mL | |
| 10 mM | 0.3980 mL | 1.9898 mL | 3.9796 mL | 9.9491 mL | |
| 15 mM | 0.2653 mL | 1.3265 mL | 2.6531 mL | 6.6327 mL | |
| 20 mM | 0.1990 mL | 0.9949 mL | 1.9898 mL | 4.9745 mL | |
| 25 mM | 0.1592 mL | 0.7959 mL | 1.5918 mL | 3.9796 mL | |
| 30 mM | 0.1327 mL | 0.6633 mL | 1.3265 mL | 3.3164 mL | |
| 40 mM | 0.0995 mL | 0.4975 mL | 0.9949 mL | 2.4873 mL |
NU6027 関連分類
HY-13816 関連分類
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