Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Purvalanol A (NG60; NG-60; NG 60) is a potent and cell-permeable CDK (cyclin-dependent kinase) inhibitor with potential antitumor activity. It has IC50 values of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1 inhibition, respectively. Purvalanol A (30 μM) caused apoptosis in MKN45 cells by downregulating the expression of the antiapoptotic proteins survivin, Bcl-XL, and Bcl-2. Additionally, purvalanol A inhibited the expression and phosphorylation of RNA polymerase II, which was involved in transcriptional regulation, as well as the phosphorylation of STAT3 by Janus kinase 2 (JAK2).
Targets |
cdc2-cyclin B (IC50 = 4 nM); cdk2-cyclin E (IC50 = 35 nM); cdk2-cyclin A (IC50 = 70 nM); cdk4-cyclin D1 (IC50 = 850 nM); cdk5-p35 (IC50 = 75 nM); erk1 (IC50 = 9000 nM)
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
Purvalanol A is a potent CDK inhibitor, inhibiting 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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Cell Assay |
In 96-well plates, cells are seeded at a density of 10,000 and exposed to different concentrations of Purvalanol A (0-100 μM) for a duration of 24 hours. For four hours, cells are incubated at 37°C after being exposed to 10 μL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye (5 mg/mL). 100 μL of DMSO is added to the formazan crystals to help them dissolve. The absorbance is measured spectrophotometrically at 570 nm.
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Animal Protocol |
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References |
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Molecular Formula |
C19H25CLN6O
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Molecular Weight |
388.89
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Exact Mass |
388.18
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Elemental Analysis |
C, 58.68; H, 6.48; Cl, 9.12; N, 21.61; O, 4.11
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CAS # |
212844-53-6
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Related CAS # |
Purvalanol B;212844-54-7
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Appearance |
Grey to green solid powder
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SMILES |
CC(C)[C@H](CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NC3=CC(=CC=C3)Cl
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InChi Key |
PMXCMJLOPOFPBT-HNNXBMFYSA-N
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InChi Code |
InChI=1S/C19H25ClN6O/c1-11(2)15(9-27)23-19-24-17(22-14-7-5-6-13(20)8-14)16-18(25-19)26(10-21-16)12(3)4/h5-8,10-12,15,27H,9H2,1-4H3,(H2,22,23,24,25)/t15-/m0/s1
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Chemical Name |
(2R)-2-[[6-(3-chloroanilino)-9-propan-2-ylpurin-2-yl]amino]-3-methylbutan-1-ol
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5714 mL | 12.8571 mL | 25.7142 mL | |
5 mM | 0.5143 mL | 2.5714 mL | 5.1428 mL | |
10 mM | 0.2571 mL | 1.2857 mL | 2.5714 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.