Purvalanol A
Based on 4 publication(s) in Google Scholar
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
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- Pureté: 98.61%
- CAS No.: 212844-53-6
- Formule: C19H25ClN6O
- Masse moléculaire:388.89
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Stockage: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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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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Publications Citing Use of MedChemExpress (MCE) Purvalanol A
More
Activité biologique
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cdc2-cyclin B 4 nM (IC50) |
cdk2-cyclin E 35 nM (IC50) |
cdk2-cyclin A 70 nM (IC50) |
cdk4-cyclin D1 850 nM (IC50) |
cdk5-p35 75 nM (IC50) |
erk1 9000 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | IC50 |
7.4 μM
Compound: Purvalanol A
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In vitro cytotoxic effect on CEM cancer cell line
In vitro cytotoxic effect on CEM cancer cell line
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[PMID: 12392733] |
| G-361 | IC50 |
24 μM
Compound: Purvalanol A
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In vitro cytotoxic effect on G361 cancer cell line
In vitro cytotoxic effect on G361 cancer cell line
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[PMID: 12392733] |
| HOS | IC50 |
22 μM
Compound: Purvalanol A
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In vitro cytotoxic effect on HOS cancer cell line
In vitro cytotoxic effect on HOS cancer cell line
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[PMID: 12392733] |
| HT-29 | IC50 |
>100 μM
Compound: purvalanol A
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Cytotoxicity against human HT-29 cells by MTT assay
Cytotoxicity against human HT-29 cells by MTT assay
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[PMID: 20804197] |
| K562 | IC50 |
9 μM
Compound: Purvalanol A
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In vitro cytotoxic effect on K562 cancer cell line
In vitro cytotoxic effect on K562 cancer cell line
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[PMID: 12392733] |
| K562 | IC50 |
9 μM
Compound: purvalanol A
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Cytotoxic property against K562 cell line was determined
Cytotoxic property against K562 cell line was determined
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[PMID: 12941319] |
| KM12 | GI50 |
76 nM
Compound: Purvalanol A
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Growth inhibition human KM12 cells
Growth inhibition human KM12 cells
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[PMID: 9677190] |
| MCF7 | IC50 |
10.7 μM
Compound: Purvalanol A
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In vitro cytotoxic effect on MCF-7 cancer cell line
In vitro cytotoxic effect on MCF-7 cancer cell line
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[PMID: 12392733] |
| MCF7 | IC50 |
10.7 μM
Compound: purvalanol A
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Cytotoxic property against MCF-7 cell line was determined
Cytotoxic property against MCF-7 cell line was determined
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[PMID: 12941319] |
| NCI-H522 | GI50 |
347 nM
Compound: Purvalanol A
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Growth inhibition human NCI-H522 cells
Growth inhibition human NCI-H522 cells
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[PMID: 9677190] |
| Oocyte | IC50 |
0.004 μM
Compound: purvalanol A
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Inhibition of starfish oocytes CDK1/cyclin B
Inhibition of starfish oocytes CDK1/cyclin B
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[PMID: 19128055] |
| Oocyte | IC50 |
4 nM
Compound: purvalanol A
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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 A inhibits cdc28 (S. cerevisiae) and erk1 with IC50s of 80 and 9000 nM. Purvalanol A shows inhibitory activities against the NCI panel of 60 human tumor cell lines, with average GI50 of 2 μM; two cell lines show an -20-fold increase in sensitivity to purvalanol A: the KM12 colon cancer cell line with a GI50 of 76 nM and the NCI-H522 non–small cell lung cancer cell line with a GI50 of 347 nM[1]. Purvalanol A is a 2.5-fold more potent inhibitor of CDK2, but also inhibits DYRK1A potently and a number of other protein kinases in the low micromolar range. Purvalanol A inhibits MKK1, MAPK2/ERK2, JNK/SAPK1c with IC50s of 80, 26, 84 μM[2]. Purvalanol A selectively inhibits the phosphorylation of cellular proteins. Purvalanol A prevents the increases of the contents of cyclins D and E during serum-induced G1 phase progression. Purvalanol A does not inhibit transcription under cell-free conditions[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 212844-53-6
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Appearance Solid
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Masse moléculaire 388.89
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Formule C19H25ClN6O
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Color Light yellow to yellow
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SMILES
CC([C@@H](NC1=NC(NC2=CC=CC(Cl)=C2)=C3N=CN(C(C)C)C3=N1)CO)C
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Synonyms
NG-60
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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 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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EMBO Rep
2022 Jun 7;23(6):e53932. PMID: 35403787 -
mBio
Functional insight into cyclin-dependent kinase (CDK)7 via chemical inhibition of the priority fungal pathogen Cryptococcus neoformans. [Abstract]2025 Dec 10;16(12):e0289825. PMID: 41171060 -
iScience
2019 May 31:15:291-306. PMID: 31102995 -
Mol Carcinog
Purvalanol A Exerts Anti-Hepatocellular Carcinoma Activity by Activating the p53 Pathway. [Abstract]2025 Dec 2. PMID: 41328606
Solvant et solubilité
DMSO : ≥ 50 mg/mL (128.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 10 mg/mL (25.71 mM; Need ultrasonic)
* "≥" 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.
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 (6.43 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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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]. Bain J, et al. The specificities of protein kinase inhibitors: an update. Biochem J. 2003 Apr 1;371(Pt 1):199-204. [Content Brief]
[3]. Villerbu N, et al. Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int J Cancer. 2002 Feb 20;97(6):761-9. [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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.5714 mL | 12.8571 mL | 25.7142 mL | 64.2855 mL |
| 5 mM | 0.5143 mL | 2.5714 mL | 5.1428 mL | 12.8571 mL | |
| 10 mM | 0.2571 mL | 1.2857 mL | 2.5714 mL | 6.4286 mL | |
| 15 mM | 0.1714 mL | 0.8571 mL | 1.7143 mL | 4.2857 mL | |
| 20 mM | 0.1286 mL | 0.6429 mL | 1.2857 mL | 3.2143 mL | |
| 25 mM | 0.1029 mL | 0.5143 mL | 1.0286 mL | 2.5714 mL | |
| DMSO | 30 mM | 0.0857 mL | 0.4286 mL | 0.8571 mL | 2.1429 mL |
| 40 mM | 0.0643 mL | 0.3214 mL | 0.6429 mL | 1.6071 mL | |
| 50 mM | 0.0514 mL | 0.2571 mL | 0.5143 mL | 1.2857 mL | |
| 60 mM | 0.0429 mL | 0.2143 mL | 0.4286 mL | 1.0714 mL | |
| 80 mM | 0.0321 mL | 0.1607 mL | 0.3214 mL | 0.8036 mL | |
| 100 mM | 0.0257 mL | 0.1286 mL | 0.2571 mL | 0.6429 mL |
Purvalanol A Related Classifications
HY-18299A Related Classifications
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