Chemical Name: 4-[2-Methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine
Biological ActivityPotent inhibitor of cyclin dependent kinases (cdks; reported IC50 values are 6 - 45, 14, 16 and 20 nM for cdk2, cdk5, cdk1 and cdk9 respectively). Also inhibits cdk4 and cdk7 in the sub micromolar range. Exhibits antiproliferative activity in human tumor cell lines. Blocks cell cycling at G2-M, S and G1 phases; reduces the proportion of actively cycling cells in vivo.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
Byth et al.
Mol.Cancer Ther., 2009;8:1856
How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
Citations for AZD 5438
The citations listed below are publications that use Tocris products. Selected citations for AZD 5438 include:
2 Citations: Showing 1 - 2
A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers.
Authors: Goonesekere Et al.
PLoS One 2014;9:e93046
Functional characterization of the 19q12 amplicon in grade III breast cancers.
Authors: Natrajan Et al.
Breast Cancer Res 2012;14:R53
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