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别名 TAS-2104, TAS2104, TAS119, TAS 2104, TAS 119
TAS-119 (TAS-2104) 是一种可口服且具有选择性和有效性的 Aurora A 抑制剂,IC50为1.0 nM。TAS-119 对 Aurora B 也具有抑制作用,IC50 为 95 nM。TAS-119 对 Aurora A 的亲和力比 Aurora B高。TAS-119 具有有效的抗肿瘤活性和潜在的抗有丝分裂活性。


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TAS-119 (TAS-2104) 是一种可口服且具有选择性和有效性的 Aurora A 抑制剂,IC50为1.0 nM。TAS-119 对 Aurora B 也具有抑制作用,IC50 为 95 nM。TAS-119 对 Aurora A 的亲和力比 Aurora B高。TAS-119 具有有效的抗肿瘤活性和潜在的抗有丝分裂活性。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 795 | 现货 | |
| 5 mg | ¥ 1,980 | 现货 | |
| 10 mg | ¥ 3,180 | 现货 | |
| 25 mg | ¥ 4,970 | 现货 | |
| 50 mg | ¥ 6,900 | 现货 | |
| 100 mg | ¥ 9,490 | 现货 | |
| 200 mg | ¥ 12,800 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 2,190 | 现货 |
| 产品描述 | TAS-119 (TAS-2104) is an orally available, selective and potent inhibitor of Aurora A with an IC50 of 1.0 nM.TAS-119 also inhibits Aurora B with an IC50 of 95 nM.TAS-119 has a higher affinity for Aurora A than for Aurora B.TAS-119 exhibits potent antitumor activity and potential antimitotic activity. TAS-119 has potent anti-tumor activity and potential anti-mitotic activity. |
| 靶点活性 | Aurora B:95 nM (IC50), Aurora A:1 nM (IC50) |
| 体外活性 | TAS-119 (30-300 nM) dose-dependently enhances cell growth inhibition by three taxanes (Paclitaxel, Docetaxel, and Cabazitaxel) in HeLa cells. TAS-119 induces mitotic accumulation predominantly in tumor cells, compared with that in normal diploid fibroblasts.[1] |
| 体内活性 | TAS-119 (5, 10, and 30 mg/kg; oral; twice daily on day 1 and every day on day 2; Nude rats injected with HeLa-luc cells) induced pHH3 at all doses in nude rats with the HeLa-luc xenografts. The treatment induces phosphorylated histone H3 (pHH3) in nude rats with the HeLa-luc xenografts.[1] |
| 别名 | TAS-2104, TAS2104, TAS119, TAS 2104, TAS 119 |
| 分子量 | 506.36 |
| 分子式 | C23H22Cl2FN5O3 |
| CAS No. | 1453099-83-6 |
| Smiles | Cc1cc(Nc2nc(CC3(CCN(CC3)C(=O)c3cccc(Cl)c3Cl)C(O)=O)ccc2F)n[nH]1 |
| 密度 | 1.31g/cm3 |
| 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: 45 mg/mL (88.87 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.95 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。 | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
对于不同动物的给药剂量换算,您也可以参考 更多