TAS-119|1453099-83-6|-陌孚医药/Medlife

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TAS-119

目录号: PL13931 纯度: ≥98%

CAS No. :1453099-83-6

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中文名称	TAS-119
中文别名	化合物 T34787
英文名称	TAS-119
英文别名	TAS-119;1-(2,3-Dichlorobenzoyl)-4-((5-fluoro-6-((5-methyl-1H-pyrazol-3-yl)amino)pyridin-2-yl)methyl)piperidine-4-carboxylic acid;1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridin-2-yl]methyl]piperidine-4-carboxylic acid;A936878;CID 71696703;4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]-;TAS 2104;TAS2104;TAS-2104;VIC-1911 (TAS-119)
Cas No.	1453099-83-6
分子式	C₂₃H₂₂Cl₂FN₅O₃
分子量	506.36
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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。

生物活性

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC 50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC 50 of 95 nM). TAS-119 has potent antitumor activites.

性状

Solid

IC50 & Target[1][2]

Aurora A 1 nM (IC50) Aurora B 95 nM (IC

体外研究(In Vitro)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Hiroshi Sootome, et al. Aurora A Inhibitor TAS-119 Enhances Antitumor Efficacy of Taxanes In Vitro and In Vivo: Preclinical Studies as Guidance for Clinical Development and Trial Design. Mol Cancer Ther. 2020 Oct;19(10):1981-1991.

溶解度数据	In Vitro: DMSO : 50 mg/mL (98.74 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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