Roscovitine

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Cat.No. 1332 - Roscovitine | CAS No. 186692-46-6
Description: Cdk inhibitor
Chemical Name: (2R)-2-[[9-(1-Methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

Cyclin-dependent kinase (cdk) inhibitor. Displays sub-micromolar inhibition of cdk1, cdk2, cdk5, cdk7 and cdk9 (reported IC50 values range from 0.16 - 0.28 μM for cdk5 to 0.8 μM for cdk7). Selective for cdks over a wide range of related kinases including ERK1 and ERK2. Arrests L1210 cells in G1 phase. Inhibits phosphorylation of vimentin in vivo. Antimitotic.

Technical Data

M. Wt 354.45
Formula C19H26N6O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 186692-46-6
PubChem ID 160355
InChI Key BTIHMVBBUGXLCJ-OAHLLOKOSA-N
Smiles OC[C@@H](CC)NC1=NC(N(C(C)C)C=N2)=C2C(NCC3=CC=CC=C3)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.44 100
ethanol 35.44 100

Preparing Stock Solutions

The following data is based on the product molecular weight 354.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.82 mL 14.11 mL 28.21 mL
5 mM 0.56 mL 2.82 mL 5.64 mL
10 mM 0.28 mL 1.41 mL 2.82 mL
50 mM 0.06 mL 0.28 mL 0.56 mL

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References

References are publications that support the biological activity of the product.

De Azevedo et al (1997) Inhibition of cyclin-dependent kinases by purine analogues. Eur.J.Biochem. 243 518 PMID: 9030780

Meijer (1996) Chemical inhibitors of cyclin-dependent kinases. Trends Cell.Biol. 6 393 PMID: 15157522

Meijer et al (1997) Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur.J.Biochem. 243 527 PMID: 9030781

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987


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Keywords: Roscovitine, Roscovitine supplier, Potent, selective, inhibitors, inhibits, cyclin, dependent, kinases, cdks, cdc2, B, cdk2, A, E, cdk5, p35, antimitotic, Cyclin-dependent, Kinase, 1332, Tocris Bioscience

Citations for Roscovitine

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