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Submit ReviewCHR 6494 trifluoroacetate is a potent and selective haspin kinase inhibitor (IC50 = 2 nM). Selective over 27 other protein kinases including Aurora B kinase. Induces cell cycle arrest at G2/M, inhibits cell proliferation and promotes apoptosis in multiple cancer cell lines. Inhibits angiogenesis ex vivo and attenuates tumor growth of HCT-116 xenografts in rats.
CHR 6494 trifluoroacetate is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 406.36 |
公式 | C16H16N6.CF3CO2H |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1458630-17-5 |
PubChem ID | 91691123 |
InChI Key | ILWYDZNXJQESDI-UHFFFAOYSA-N |
Smiles | CCCNC2=NN1C(C3=CC(C=NN4)=C4C=C3)=CN=C1C=C2.OC(C(F)(F)F)=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 | 40.64 | 100 |
以下数据基于产品分子量 406.36。 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 | 2.46 mL | 12.3 mL | 24.61 mL |
5 mM | 0.49 mL | 2.46 mL | 4.92 mL |
10 mM | 0.25 mL | 1.23 mL | 2.46 mL |
50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
参考文献是支持产品生物活性的出版物。
Huertas et al (2012) Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene 31 1408 PMID: 21804608
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关键词: CHR 6494 trifluoroacetate, CHR 6494 trifluoroacetate supplier, CHR6494, trifluoroacetate, potent, selective, haspin, kinases, inhibitors, inhibits, cell, cycle, arrest, proliferation, apoptosis, GSG2, Haspin, 5326, Tocris Bioscience
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*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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.