PURVALANOL A Chemical Properties

Boiling point:

590.5±60.0 °C(Predicted)

Density 

1.33±0.1 g/cm3(Predicted)

storage temp. 

Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

solubility 

methylene chloride: 50 mg/mL, clear, colorless

form 

powder

pka

14.51±0.10(Predicted)

color 

off-white

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

Safety Information

WGK Germany 

3

HS Code 

2933599590

MSDS

• Language:English Provider:SigmaAldrich

PURVALANOL A Usage And Synthesis

Description

Purvalanol A (212844-53-6) is a cyclin-dependent kinase inhibitor. IC50s= 4, 70, 35, 75 and 850 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk5/p35 and cdk4/cyclin D1 and respectively.1?Reversibly arrests synchronized cells in G1 and G2 phase.2?Induces ER stress-mediated apoptosis and autophagy in colon cancer cells.3?Suppresses Src-mediated transformation by inhibiting both CDKs and c-Src.4?In cells transformed with MYC, purvalanol A rapidly down-regulates survivin expression and induces MYC-dependent apoptosis.5?Cell permeable.

Uses

Purvalanol A acts as a potent, cell-permeable CDK inhibitor used in the treatment of cell proliferative disorders. Anti-cancer.

Definition

ChEBI: Purvalanol A is a purvalanol.

Biological Activity

Cyclin-dependent kinase inhibitor. IC 50 values are 4, 70, 35, 850 and 75 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. Reversibly arrests synchronised cells in G1 and G2, and inhibits cell proliferation and cell death.

storage

Store at +4°C

References

[1] SERA T. [Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors].[J]. Tanpakushitsu kakusan koso. Protein, nucleic acid, enzyme, 2007, 52 13 Suppl: 1812-1813.
[2] NATHALIE VILLERBU. Cellular effects of purvalanol A: A specific inhibitor of cyclin-dependent kinase activities[J]. International Journal of Cancer, 2001, 97 6: 761-769. DOI:10.1002/ijc.10125
[3] AJDA COKER-GÜRKAN. Purvalanol induces endoplasmic reticulum stress-mediated apoptosis and autophagy in a time-dependent manner in HCT116 colon cancer cells.[J]. Oncology reports, 2015: 2761-2770. DOI:10.3892/or.2015.3918
[4] TOMOYA HIKITA  Masato O  Chitose Oneyama. Purvalanol A, a CDK inhibitor, effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src.[J]. Genes to Cells, 2010, 15 10: 1051-1062. DOI:10.1111/j.1365-2443.2010.01439.x
[5] ANDREI GOGA. Inhibition of CDK1 as a potential therapy for tumors over-expressing MYC[J]. Nature Medicine, 2007, 13 7: 820-827. DOI:10.1038/nm1606

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