A selective CDK inhibitor
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Aminopurvalanol A

Item No. 21424

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2R)-2-[[6-[(3-amino-5-chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanol
CAS Number
220792-57-4
Synonyms
  • NG 97
Molecular Formula
C19H26ClN7O
Formula Weight
403.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMF:PBS (pH 7.2) (1:5): 0.2 mg/mlDMSO: 30 mg/mlEthanol: 10 mg/ml
λmax
211, 256, 315 nm
SMILES
CC(C)N1C2=NC(N[C@H](C(C)C)CO)=NC(NC3=CC(Cl)=CC(N)=C3)=C2N=C1
InChi Code
InChI=1S/C19H26ClN7O/c1-10(2)15(8-28)24-19-25-17(23-14-6-12(20)5-13(21)7-14)16-18(26-19)27(9-22-16)11(3)4/h5-7,9-11,15,28H,8,21H2,1-4H3,(H2,23,24,25,26)/t15-/m0/s1
InChi Key
RAMROQQYRRQPDL-HNNXBMFYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $63

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    5 mg

    $197

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    Product Description

    Aminopurvalanol A is a selective, cell-permeable, and competitive cyclin-dependent kinase (CDK) inhibitor that potently inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p35 (IC50s = 33, 33, 28, and 20 nM, respectively).1 It is over 90-fold selective for CDKs over ERK1, ERK2, PKC-δ, protein kinase A (PKA), casein kinase 1, insulin receptor tyrosine kinase (IC50s = 3.0-36 μM), and over 3,000-fold selective over a range of other kinases (IC50s > 100 μM). In antiproliferative assays in vitro, aminopurvalanol A inhibits growth of ovarian (IGROV1), leukemic (SR), lung (NCI-H522), and colonic (KM12) cells (GI50s = 470, 420, 1,000, and 30 nM, respectively). Aminopurvalanol A also inhibits mitotic division and preferentially arrests cells in the G2/M phase via Cdk1/cyclin B2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chang, Y.-T., Gray, N.S., Rosania, G.R., et al. Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors. Chem. Biol. 6(6), 361-375 (1999).

    2. Rosania, G.R., Merlie, J.J., Gray, N., et al. A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts. Proc. Natl. Acad. Sci. USA 96(9), 4797-4802 (1999).

    3. Knockaert, M., Gray, N., Damiens, E., et al. Intracellular targets of cyclin-dependent kinase inhibitors: identification by affinity chromatography using immobilised inhibitors. Chem. Biol. 7(6), 411-422 (2000).