A potent inhibitor of CDKs
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AZD 5438

Item No. 21598

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine
CAS Number
602306-29-6
Molecular Formula
C18H21N5O2S
Formula Weight
371.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 0.2 mg/ml
λmax
300 nm
SMILES
CS(C1=CC=C(NC2=NC(C3=CN=C(C)N3C(C)C)=CC=N2)C=C1)(=O)=O
InChi Code
InChI=1S/C18H21N5O2S/c1-12(2)23-13(3)20-11-17(23)16-9-10-19-18(22-16)21-14-5-7-15(8-6-14)26(4,24)25/h5-12H,1-4H3,(H,19,21,22)
InChi Key
WJRRGYBTGDJBFX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $98

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    10 mg

    $185

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    25 mg

    $412

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    50 mg

    $722

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    Product Description

    AZD 5438 is a potent inhibitor of the cyclin-dependent kinases (CDKs) 1, 2, and 9 (IC50s = 16, 6, and 20 nM, respectively).1 AZD 5438 also inhibits the kinase activity of Cdk5/p25 and glycogen synthase kinase 3β (GSK3β) (IC50s = 14 and 17 nM, respectively). AZD 5438 induces cell cycle arrest by inhibiting phosphorylation of CDK-dependent substrates and exhibits in vitro antiproliferative activity against a range of tumor cell lines including lung, colorectal, breast, prostate, and hematologic tumors with IC50s ranging from 200 nM (MCF-7) to 1,700 nM (ARH-77).1,2 AZD 5438 inhibits growth of human tumor xenografts derived from a wide range of cancer types and inhibits cell cycle proteins.1,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Byth, K.F., Thomas, A., Hughes, G., et al. AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. Mol. Cancer. Ther. 8(7), 1856-1866 (2009).

    2. Raghavan, P., Tumati, V., Yu, L., et al. AZD5438, an inhibitor of Cdk1, 2, and 9, enhances the radiosensitivity of non-small cell lung carcinoma cells. Int. J. Radiat. Oncol. Biol. Phys. 84(4), e507-e514 (2012).

    3. Dickson, M.A., and Schwartz, G.K. Development of cell-cycle inhibitors for cancer therapy. Curr. Oncol. 16(2), 36-43 (2009).