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。
货号:ajcx33808
CAS:1453099-83-6
分子式:C23H22Cl2FN5O3
分子量：506.36
溶解度:DMSO : 50 mg/mL (98.74 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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[1].

TAS-119 enhances the antiproliferative effect of Paclitaxel in a variety of human cancer cell lines, including Paclitaxel-resistant cells[1].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 (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[1].

[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.