TAS-119

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TAS-119 是一种有效的，选择性的，具有口服活性的 Aurora A 抑制剂，IC50 为 1.0 nM。TAS-119 对 Aurora A 的选择性高于其他蛋白激酶，包括 Aurora B (IC50 为 95 nM)。TAS-119 具有有效的抗肿瘤活性。

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.

TAS-119 enhances the antiproliferative effect of Paclitaxel in a variety of human cancer cell lines, including Paclitaxel-resistant cells.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.

TAS-119 (5-30 mg/kg; oral administration; twice daily on day 1 and everyday on day 2) treatment induces phosphorylated histone H3 (pHH3) in nude rats with the HeLa-luc xenografts.Animal Model:Nude rats injected with HeLa-luc cells Dosage:5 mg/kg, 10 mg/kg, and 30 mg/kg Administration:Oral administration; twice daily on day 1 and everyday on day 2 Result:Induced pHH3 at all doses in nude rats with the HeLa-luc xenografts.

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Cell Cycle/DNA Damage

Aurora Kinase

Aurora Kinase

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1453099-83-6

506.36

C23H22Cl2FN5O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (98.74 mM; 超声助溶 )

Cc1cc(Nc2nc(CC3(CCN(CC3)C(=O)c3cccc(Cl)c3Cl)C(O)=O)ccc2F)n[nH]1

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(-20℃)

With Ice Pack

≥ 2 years