产品
编 号：F741219
分子式：C23H22Cl2FN5O3
分子量：506.36
分子式：C23H22Cl2FN5O3
分子量：506.36
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
10mg
询价
询价
25mg
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询价
结构图
CAS No: 1453099-83-6
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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 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.
体内研究：
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.
体外研究：
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.
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