Purvalanol B
Based on 2 publication(s) in Google Scholar
Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum.
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- 純度: 97.0%
- CAS 番号: 212844-54-7
- 分子式: C20H25ClN6O3
- 分子量:432.90
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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
- 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 Purvalanol B
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生物活性
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cdc2/cyclin B 6 nM (IC50) |
cdk2/cyclin A 6 nM (IC50) |
CDK2/cyclinE 9 nM (IC50) |
CDK5/p35 6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| MCF7 | IC50 |
>100 μM
Compound: Purvalanol B
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Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by WST-1 assay
Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by WST-1 assay
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[PMID: 21440449] |
| MDA-MB-231 | IC50 |
>100 μM
Compound: Purvalanol B
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Antiproliferative activity against estrogen receptor-deficient human MDA-MB-231 cells after 48 hrs by WST-1 assay
Antiproliferative activity against estrogen receptor-deficient human MDA-MB-231 cells after 48 hrs by WST-1 assay
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[PMID: 21440449] |
| Oocyte | IC50 |
6 nM
Compound: purvalanol B
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In vitro inhibitory activity against Cyclin-dependent kinase 1-cyclin B complex from starfish oocytes
In vitro inhibitory activity against Cyclin-dependent kinase 1-cyclin B complex from starfish oocytes
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[PMID: 10753466] |
Purvalanol B binds to P. falciparum casein kinase 1 (CK1) from blood stage cell lysates and inhibits the growth a chloroquine-resistant strain of P. falciparum (FCR-3) with an IC50 of 7.07 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 212844-54-7
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性状 Solid
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分子量 432.90
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分子式 C20H25ClN6O3
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Color White to light yellow
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SMILES
O=C(O)C1=CC=C(NC2=C3N=CN(C(C)C)C3=NC(N[C@@H](CO)C(C)C)=N2)C=C1Cl
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別名
NG 95
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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 (2)
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Journal Impact Factor
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Most Recent
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Anticancer Drugs
2023 Jan 1;34(1):29-43. PMID: 35946506 -
溶剤 & 溶解度
DMSO : ≥ 40 mg/mL (92.40 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (5.78 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.
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 (277 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Gray NS, et, al. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8. [Content Brief]
[2]. Bullard KM, et, al. Effects of cyclin-dependent kinase inhibitor Purvalanol B application on protein expression and developmental progression in intra-erythrocytic Plasmodium falciparum parasites. Malar J. 2015 Apr 8;14:147. [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, 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 | 2.3100 mL | 11.5500 mL | 23.1000 mL | 57.7501 mL |
| 5 mM | 0.4620 mL | 2.3100 mL | 4.6200 mL | 11.5500 mL | |
| 10 mM | 0.2310 mL | 1.1550 mL | 2.3100 mL | 5.7750 mL | |
| 15 mM | 0.1540 mL | 0.7700 mL | 1.5400 mL | 3.8500 mL | |
| 20 mM | 0.1155 mL | 0.5775 mL | 1.1550 mL | 2.8875 mL | |
| 25 mM | 0.0924 mL | 0.4620 mL | 0.9240 mL | 2.3100 mL | |
| 30 mM | 0.0770 mL | 0.3850 mL | 0.7700 mL | 1.9250 mL | |
| 40 mM | 0.0578 mL | 0.2888 mL | 0.5775 mL | 1.4438 mL | |
| 50 mM | 0.0462 mL | 0.2310 mL | 0.4620 mL | 1.1550 mL | |
| 60 mM | 0.0385 mL | 0.1925 mL | 0.3850 mL | 0.9625 mL | |
| 80 mM | 0.0289 mL | 0.1444 mL | 0.2888 mL | 0.7219 mL |
Purvalanol B 関連分類
HY-18299 関連分類
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