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Submit ReviewAZD 5438 is a 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.
Sold with the permission of AstraZeneca UK Ltd.
AZD 5438 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 371.46 |
公式 | C18H21N5O2S |
储存 | Desiccate at RT |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 37.15 | 100 |
以下数据基于产品分子量 371.46。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for AZD 5438, please let us know.
关键词: AZD 5438, AZD 5438 supplier, AZD5438, Cdk, inhibitor, cyclin-dependent, kinase, inhibitors, inhibits, cdk1, cdk2, cdk9, Cell, Cycle, Inhibitors, Cyclin-dependent, Kinase, Non-selective, CDKs, 3968, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AZD 5438 的部分引用包括:
Cheng et al (2022) Translational and post-translational control of human naïve versus primed pluripotency. iScience 25 103645 PMID: 35005567
Natrajan et al (2012) Functional characterization of the 19q12 amplicon in grade III breast cancers. Breast Cancer Res 14 R53 PMID: 22433433
Helen et al (2023) AZD5438 a GSK-3a/b and CDK inhibitor is antiapoptotic modulates mitochondrial activity and protects human neurons from mitochondrial toxins. Sci Rep 13 8334 PMID: 37221196
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
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