A CDK inhibitor
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Dinaciclib

Item No. 14707

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[3-ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]-2S-piperidineethanol
CAS Number
779353-01-4
Synonyms
  • SCH 727965
Molecular Formula
C21H28N6O2
Formula Weight
396.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 15 mg/mlEthanol: 25 mg/ml
λmax
216, 259 nm
SMILES
OCC[C@H]1N(C2=NC3=C(CC)C=NN3C(NCC4=CC=C[N+]([O-])=C4)=C2)CCCC1
InChi Code
InChI=1S/C21H28N6O2/c1-2-17-14-23-27-19(22-13-16-6-5-9-25(29)15-16)12-20(24-21(17)27)26-10-4-3-7-18(26)8-11-28/h5-6,9,12,14-15,18,22,28H,2-4,7-8,10-11,13H2,1H3/t18-/m0/s1
InChi Key
PIMQWRZWLQKKBJ-SFHVURJKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $103

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    10 mg

    $194

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    25 mg

    $454

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    Product Description

    Cyclin-dependent kinases (CDKs) are critical positive regulators of cell cycle progression and cellular transcription whose dysregulation can lead to the development of cancer. Dinaciclib inhibits CDK1, CDK2, CDK5, and CDK9 activity in vitro with IC50 values of 3, 1, 1, and 4 nM, respectively.1 Compared to the pan-CDK inhibitor flavopiridol (Item No. 10009197), dinaciclib is an equally potent inhibitor of CDK1 and CDK9 but a 12-14-fold more potent inhibitor of CDK2 and CDK5.1 It has been shown to inhibit DNA synthesis by blocking thymidine incorporation in A2780 ovarian cancer cells with an IC50 value of 4 nM.1 At 5 mg/kg it prevents tumor growth by 50% in an A2780 ovarian carcinoma mouse xenograft model and is active against a broad spectrum of human tumor cell lines in vitro (IC50s = 7-17 nM).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Parry, D., Guzi, T., Shanahan, F., et al. Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol. Cancer Ther. 9(8), 2344-2353 (2010).