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Submit ReviewAZ 3146
说明： Potent and selective Mps1 kinase inhibitor
化学名： 9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one
纯度： ≥99% (HPLC)
生物活性 for AZ 3146
AZ 3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM). Displays selectivity over 46 other kinases including Cdk1 and aurora kinase B. Interferes with chromosome alignment and overrides spindle assembly checkpoint. Inhibits the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores.
许可信息
Sold for research purposes only under agreement from AstraZeneca UK Ltd.
化合物库 for AZ 3146
AZ 3146 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。
技术数据 for AZ 3146
| 分子量 | 452.55 |
| 公式 | C24H32N6O3 |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1124329-14-1 |
| PubChem ID | 56973724 |
| InChI Key | YUKWVHPTFRQHMF-UHFFFAOYSA-N |
| Smiles | CN(C1=CN=C(NC4=CC=C(OC5CCN(C)CC5)C=C4OC)N=C1N2C3CCCC3)C2=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.
溶解性数据 for AZ 3146
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 11.31 | 25 | |
| ethanol | 33.94 | 75 |
制备储备液 for AZ 3146
以下数据基于产品分子量 452.55。 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 |
|---|---|---|---|
| 0.75 mM | 2.95 mL | 14.73 mL | 29.46 mL |
| 3.75 mM | 0.59 mL | 2.95 mL | 5.89 mL |
| 7.5 mM | 0.29 mL | 1.47 mL | 2.95 mL |
| 37.5 mM | 0.06 mL | 0.29 mL | 0.59 mL |
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产品说明书 for AZ 3146
参考文献 for AZ 3146
参考文献是支持产品生物活性的出版物。
Hewitt et al (2010) Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J.Cell Biol. 190 25 PMID: 20624899
Lan and Cleveland (2010) A chemical tool box defines mitotic and interphase roles for Mps1 kinase. J.Cell.Biol. 190 21 PMID: 20624898
Maciejowski et al (2010) Mps1 directs the assembly of Cdc20 inhbitory complexes during interphase and mitosis to control M phase timing and spindle checkpoint signaling. J.Cell Biol. 190 89 PMID: 20624902
If you know of a relevant reference for AZ 3146, please let us know.
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关键词: AZ 3146, AZ 3146 supplier, AZ, astrazeneca, Mps1, monopolar, spindle, selective, potent, inhibitors, inhibits, SAC, assembly, checkpoint, control, TTK, dual-specificity, protein, kinases, kinetochores, CENP-E, centromere, E, AZ3146, Checkpoint, Control, Kinases, Monopolar, Spindle, 1, Kinase, 3994, Tocris Bioscience
13 篇 AZ 3146 的引用文献
引用文献是使用了 Tocris 产品的出版物。 AZ 3146 的部分引用包括：
Littler et al (2019) Oncogenic MYC amplifies mitotic perturbations. Open Biol 9 190136 PMID: 31455158
Garvanska et al (2016) Synergistic inhibition of the APC/C by the removal of APC15 in HCT116 cells lacking UBE2C. Biol Open 5 1441 PMID: 27591192
Haase et al (2017) Distinct Roles of the Chromosomal Passenger Complex in the Detection of and Response to Errors in Kinetochore-Microtubule Attachment. Dev Cell 42 640 PMID: 28950102
Bennett et al (2015) Cenp-E inhibitor GSK923295: Novel synthetic route and use as a tool to generate aneuploidy. Toxins (Basel) 6 20921 PMID: 26320186
Hermant et al (2013) Amitozyn impairs chromosome segregation and induces apoptosis via mitotic checkpoint activation. PLoS One 8 e57461 PMID: 23505430
Joana C et al (2020) Small-molecule inhibition of aging-associated chromosomal instability delays cellular senescence. EMBO Rep 21 e49248 PMID: 32134180
Shabaz et al (2020) Ordered dephosphorylation initiated by the selective proteolysis of cyclin B drives mitotic exit. Elife 9 PMID: 32869743
Drpic et al (2018) Chromosome Segregation Is Biased by Kinetochore Size. Curr Biol 28 1344 PMID: 29706521
McKinley et al (2018) Cellular aspect ratio and cell division mechanics underlie the patterning of cell progeny in diverse mammalian epithelia. Elife 7 PMID: 29897330
Jun et al (2021) Separase cleaves the kinetochore protein Meikin at the meiosis I/II transition. Dev Cell 56 2192-2206.e8 PMID: 34331869
Karki (2017) Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay. Nat Commun 8 15803 PMID: 28607478
Jing et al (2018) Methods for High-throughput Drug Combination Screening and Synergy Scoring. Methods Mol Biol 1711 351-398 PMID: 29344898
Iain M et al (2017) Large-Scale Analysis of CRISPR/Cas9 Cell-Cycle Knockouts Reveals the Diversity of p53-Dependent Responses to Cell-Cycle Defects. Dev Cell 40 405-420.e2 PMID: 28216383
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Cell Cycle and DNA Damage Research Product Guide
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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. 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.