Purvalanol A

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Technical Data

Molecular Weight 388.89 Storage powder
Formula

C19H25ClN6O

in solvent
CAS No. 212844-53-6 Synonyms N/A
Solubility (25°C) * In vitro DMSO 60 mg/mL warmed (154.28 mM)
Ethanol 13 mg/mL warmed (33.42 mM)
Water Insoluble
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name (R)-2-(6-(3-chlorophenylamino)-9-isopropyl-9H-purin-2-ylamino)-3-methylbutan-1-ol

Biological Activity

Description Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively.
Targets
Cdc2/CyclinB [1]
()
CDK2/CyclinE [1] CDK2/CyclinA [1] CDK4/CyclinD1 [1]
4 nM 35 nM 70 nM 850 nM
In vitro Purvalanol A decreases cell viability in dose-dependent manner in MCF-7 and MDA-MB-231 cell lines. Purvalanol A induces cell viability loss by 50 % in MCF-7 cells but MDA-MB-231 cells sre less sensitive to Purvalanol A (32 % decreases in cell viability). Purvalanol A induces mitochondria-mediated apoptosis in MCF-7 and MDA-MB-231 cells.[2] Purvalanol A effectively prevents c-Src-mediated transformation by inhibiting both cell cycle progression and c-Src signaling, and effectively suppresses the anchorage independent growth of some human cancer cells in which c-Src is up-regulated. Purvalanol A has a stronger inhibitory effect on the anchorage-independent growth of HT29 and SW480 human colon cancer cells. [3]
In vivo
Features  

Protocol (Only for Reference)

Cell Assay: [2]

Cell lines MCF-7 and MDA-MB 231 breast cancer cells
Concentrations 100 μM
Incubation Time 24 h
Method Cells are seeded at 10000 density in 96-well plates and treated with various concentrations of Purvalanol A (0-100 μM) for 24 h. Cells are exposed to 10 μL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltet- razolium bromide dye (5 mg/mL) and are incubated at 37℃ for 4 h. In order to solubilize the formazan crystals 100 μL DMSO is added. Absorbance is determined at 570 nm spectrophotometrically.
 

References

Customer Product Validation

Data from [Data independently produced by , , J Biol Chem, 2016, 291(28):14761-72.]

(A)HeLa cells were treated with Nocodazole for 8 hours and then fixed. Before the cells were stained with phospho-specific antibody against S119 of Ajuba, they were pre-incubated with PBS (no peptide control), or non-phosphorylated (control) peptide, or the phosphorylated peptide used for immunizing rabbits. CDK1 inhibitors Purvalanol A (10 μM) together with MG132 (25 μM) were added 2 h before the cells were fixed (bottom two rows).(B)Experiments were done similarly as in (A) with phospho-specific antibody against Ser175 of Ajuba.

Purvalanol A has been referenced in 1 publications.

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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