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TAK-960 是选择性的 polo 样激酶 1 口服有效抑制剂,IC50为 0.8 nM,对 PLK2 和 PLK3 也有抑制作用,IC50分别为 16.9 和 50.2 nM。它抑制多种肿瘤细胞系的增殖,可治疗多种肿瘤异种移植。

TAK-960 是选择性的 polo 样激酶 1 口服有效抑制剂,IC50为 0.8 nM,对 PLK2 和 PLK3 也有抑制作用,IC50分别为 16.9 和 50.2 nM。它抑制多种肿瘤细胞系的增殖,可治疗多种肿瘤异种移植。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 490 | In stock | |
| 5 mg | ¥ 987 | In stock | |
| 10 mg | ¥ 1,490 | In stock | |
| 25 mg | ¥ 2,720 | In stock | |
| 50 mg | ¥ 3,970 | In stock | |
| 100 mg | ¥ 5,790 | In stock | |
| 200 mg | ¥ 7,880 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 1,270 | In stock |
TAK-960 相关产品
| 产品描述 | TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively. |
| 靶点活性 | PLK2:16.9 nM, FES/FPS:58.2 nM, PTK2/FAK:19.6 nM, PLK1:0.8 nM, PLK3:50.2 nM, MLCK/MYLK:25.6 nM |
| 体外活性 | CRC cell lines demonstrated a variable anti-proliferative response to TAK-960 with IC50 values ranging from 0.001 to >?0.75 μmol/L. Anti-proliferative effects were sustained after removal of drug. Following TAK-960 treatment a highly variable accumulation of mitotic (indicating cell cycle arrest) and apoptotic markers was observed. TAK-960 treatment induced G2/M arrest and polyploidy. Six out of the eighteen PDX models responded to single agent TAK-960 therapy (TGII<?20). The addition of TAK-960 to standard of care chemotherapy resulted in largely additive antitumor effects[1]. |
| 细胞实验 | Fifty-five CRC cell lines and 18 PDX models were exposed to TAK-960 and evaluated for proliferation (IC50) and Tumor Growth Inhibition Index, respectively.?Additionally, 2 KRAS wild type and 2 KRAS mutant PDX models were treated with TAK-960 as single agent or in combination with cetuximab or irinotecan.?TAK-960 mechanism of action was elucidated through immunoblotting and cell cycle analysis[1]. |
| 分子量 | 561.6 |
| 分子式 | C27H34F3N7O3 |
| CAS No. | 1137868-52-0 |
| Smiles | COc1cc(C(=O)NC2CCN(C)CC2)c(F)cc1Nc1ncc2N(C)C(=O)C(F)(F)CN(C3CCCC3)c2n1 |
| 密度 | 1.39 g/cm3 (Predicted) |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 35 mg/mL (62.32 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.78 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||
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DMSO
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