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Submit ReviewTAK 960 hydrochloride is a potent PLK1 inhibitor (IC50 values are 0.8, 16.9 and 50.2 nM for PLK1, PLK2 and PLK3 respectively). Exhibits >20-fold selectivity for PLK1 over FAK, MLCK and FES, and has minimal activity against a panel of 282 other kinases. Inhibits proliferation of a range of cancer cell lines in vitro and inhibits tumor growth of multiple human cancer cell xenografts in vivo. Orally bioavailable.
TAK 960 hydrochloride 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 | 598.06 |
公式 | C27H34F3N7O3.HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2108449-45-0 |
PubChem ID | 91826087 |
InChI Key | QZBHDFGFNVMONB-UHFFFAOYSA-N |
Smiles | O=C1C(F)(F)CN(C3CCCC3)C(N=C(NC4=CC(F)=C(C(NC5CCN(C)CC5)=O)C=C4OC)N=C2)=C2N1C.Cl |
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 | 59.81 | 100 |
以下数据基于产品分子量 598.06。 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 | 1.67 mL | 8.36 mL | 16.72 mL |
5 mM | 0.33 mL | 1.67 mL | 3.34 mL |
10 mM | 0.17 mL | 0.84 mL | 1.67 mL |
50 mM | 0.03 mL | 0.17 mL | 0.33 mL |
参考文献是支持产品生物活性的出版物。
Hikichi et al (2012) TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. Mol.Cancer Ther. 11 700 PMID: 22188812
Nie et al (2013) Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1). Bioorg.Med.Chem.Lett. 23 3662 PMID: 23664874
If you know of a relevant reference for TAK 960 hydrochloride, please let us know.
关键词: TAK 960 hydrochloride, TAK 960 hydrochloride supplier, TAK960, hydrochloride, potent, PLK1, inhibitors, inhibits, selective, orally, bioavailable, antitumor, 1137868520, Polo-like, Kinase, Mitosis, 5403, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 TAK 960 hydrochloride 的部分引用包括:
Marc R et al (2023) Predicting anti-cancer drug combination responses with a temporal cell state network model. PLoS Comput Biol 19 e1011082 PMID: 37126527
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