TAS-119 |
| Catalog No.GC62482 |
TAS-119 es un inhibidor de Aurora A potente, selectivo y activo por vÍa oral con una IC50 de 1,0 nM. TAS-119 muestra una alta selectividad por Aurora A sobre otras proteÍnas quinasas, incluida Aurora B (IC50 de 95 nM). TAS-119 tiene potentes actividades antitumorales.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1453099-83-6
Sample solution is provided at 25 µL, 10mM.
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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.
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