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ProductsBack/Purvalanol A [212844-53-6]
Chemical Structure
Chemical Structure
Chemical Structure

Purvalanol A [212844-53-6]

Research Use Only
AG-CR1-2903
AdipoGen Life Sciences
CAS Number212844-53-6
DownloadMSDS
Product group Chemicals
Estimated Purity>98%
Molecular Weight388.9
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    Purvalanol A [212844-53-6]
  • Delivery Days Customer
    10
  • CAS Number
    212844-53-6
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Molecular Formula
    C19H25ClN6O
  • Molecular Weight
    388.9
  • Scientific Description
    Chemical. CAS: 212844-53-6. Formula: C19H25ClN6O. MW: 388.9. Synthetic. Potent, cell permeable cyclin-dependent protein kinase (cdk) inhibitor. Inhibits human CDK1 (IC50=4nM), CDK2/cyclin A (IC50=70nM), Cdc2/cyclin B, CDK2/cyclin E (IC50=35nM), CDK4/cyclin D1 (IC50=850nM) as well as CDK5/p35 (IC50=75nM). DYRK1A inhibitor (IC50=300nM). Anticancer agent. Strong apoptotic and autophagy inducer which causes cell cycle arrest in the G1 and G2 phase in various cancer cell lines. More membrane permeable than purvalanol B. Shown to inhibit ABCB1 and ABCB2 transporters and useful in co-treatment with selected anticancer drugs. - Potent, cell permeable cyclin-dependent protein kinase (cdk) inhibitor. Inhibits human CDK1 (IC50=4nM), CDK2/cyclin A (IC50=70nM), Cdc2/cyclin B, CDK2/cyclin E (IC50=35nM), CDK4/cyclin D1 (IC50=850nM) as well as CDK5/p35 (IC50=75nM). DYRK1A inhibitor (IC50=300nM). Anticancer agent. Strong apoptotic and autophagy inducer which causes cell cycle arrest in the G1 and G2 phase in various cancer cell lines. More membrane permeable than purvalanol B. Shown to inhibit ABCB1 and ABCB2 transporters and useful in co-treatment with selected anticancer drugs.
  • SMILES
    ClC1=CC=CC(NC2=C3C(N(C(C)C)C=N3)=NC(N[C@@H](CO)C(C)C)=N2)=C1
  • Storage Instruction
    -20°C,2°C to 8°C
  • UNSPSC
    51202000

References

  • Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors: N.S. Gray, et al.; Science 281, 533 (1998)
  • The specificities of protein kinase inhibitors: An update: J. Bain, et al.; Biochem. J. 371, 199 (2003)
  • Cellular effects of purvalanol A: A specific inhibitor of cyclin-dependent kinase activities: N. Villerbu, et al.; Int. J. Cancer 97, 761 (2002)
  • Purvalanol A induces apoptosis and downregulation of antiapoptotic proteins through abrogation of phosphorylation of JAK2/STAT3 and RNA polymerase II: D. Iizuka, et al.; Anticancer Drugs 19, 565 (2008)
  • Purvalanol A, a CDK inhibitor, effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src: T. Hikita, et al.; Genes to Cells 15, 1051 (2010)
  • Olomoucine II and purvalanol A inhibit ABCG2 transporter in vitro and in situ and synergistically potentiate cytostatic effect of mitoxantrone: J. Hofman, et al.; Pharmacol. Res. 65, 312 (2012)
  • Purvalanol A, olomoucine II and roscovitine inhibit ABCB1 transporter and synergistically potentiate cytotoxic effects of daunorubicin in vitro: D. Cihalova, et al.; PLoS One 8, e83467 (2013)
  • Purvalanol induces endoplasmic reticulum stress-mediated apoptosis and autophagy in a time-dependent manner in HCT116 colon cancer cells: A. Coker-Gurkan, et al.; Oncol. Rep. 33, 2761 (2015)