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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。
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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] TAS-119 enhances the antiproliferative effect of Paclitaxel in a variety of human cancer cell lines, including Paclitaxel-resistant cells.[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 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 45 mg/mL (88.87 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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