A potent inhibitor of cyclin-dependent kinase 2
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(R)-Roscovitine

Item No. 10009569

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[9-(1-methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol
CAS Number
186692-46-6
Synonyms
  • Seliciclib
Molecular Formula
C19H26N6O
Formula Weight
354.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 50 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
231, 291 nm
SMILES
CC(C)N(C=N1)C2=C1C(NCC3=CC=CC=C3)=NC(N[C@@H](CO)CC)=N2
InChi Code
InChI=1S/C19H26N6O/c1-4-15(11-26)22-19-23-17(20-10-14-8-6-5-7-9-14)16-18(24-19)25(12-21-16)13(2)3/h5-9,12-13,15,26H,4,10-11H2,1-3H3,(H2,20,22,23,24)/t15-/m1/s1
InChi Key
BTIHMVBBUGXLCJ-OAHLLOKOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    Product Description

    (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.1 It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.2,1,3 (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.1 In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. McClue, S.J., Blake, D., Clarke, R., et al. In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine). Int. J. Cancer 102, 463-468 (2002).

    2. Meijer, L., Borgne, A., Mulner, O., et al. Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur. J. Biochem. 243, 527-536 (1997).

    3. Havlícek, L., Hanus, J., Vesely, J., et al. Cytokinin-derived cyclin-dependent kinase inhibitors: Synthesis and cdc2 inhibitory activity of olomoucine and related compounds. J. Med. Chem. 40, 408-412 (1997).

    4. Bukanov, N.O., Smith, L.A., Klinger, K.W., et al. Long-lasting arrest of murine polycystic kiney disease with CDK inhibitor roscovitine. Nature 444, 949-952 (2006).