AZD 5438

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Cat.No. 3968 - AZD 5438 | C18H21N5O2S | CAS No. 602306-29-6
Description: Cdk inhibitor; potently inhibits cdk1, 2, 5 and 9
Chemical Name: 4-[2-Methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine
Purity: ≥99% (HPLC)
Datasheet
Citations (2)
Reviews
Literature

Biological Activity

Potent 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.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Compound Libraries

AZD 5438 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 371.46
Formula C18H21N5O2S
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 602306-29-6
PubChem ID 16747683
InChI Key WJRRGYBTGDJBFX-UHFFFAOYSA-N
Smiles CS(C(C=C3)=CC=C3NC1=NC(C2=CN=C(C)N2C(C)C)=CC=N1)(=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 37.15 100

Preparing Stock Solutions

The following data is based on the product molecular weight 371.46. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.69 mL 13.46 mL 26.92 mL
5 mM 0.54 mL 2.69 mL 5.38 mL
10 mM 0.27 mL 1.35 mL 2.69 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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References

References are publications that support the biological activity of the product.

Byth et al (2009) 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 1856 PMID: 19509270

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987


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View Related Products by Product Action

View all Cyclin-Dependent Protein Kinase Inhibitors

Keywords: AZD 5438, AZD 5438 supplier, AZD5438, Cdk, inhibitor, cyclin-dependent, kinase, inhibitors, inhibits, cdk1, cdk2, cdk9, Cyclin-dependent, Kinase, Cell, Cycle, Inhibitors, 3968, Tocris Bioscience

2 Citations for AZD 5438

Citations are publications that use Tocris products. Selected citations for AZD 5438 include:

Goonesekere et al (2014) A meta analysis of pancreatic microarray datasets yields new targets as cancer genes and biomarkers. PLoS One 9 e93046 PMID: 24740004

Natrajan et al (2012) Functional characterization of the 19q12 amplicon in grade III breast cancers. Breast Cancer Res 14 R53 PMID: 22433433


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Literature in this Area

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Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.