Chemical Structure : TAS-119
CAS No.: 1453099-83-6
Catalog No.: PC-72439Not For Human Use, Lab Use Only.
TAS-119 (TAS119) is a potent, selective, orally active inhibitor of Aurora A with IC50 of 1 nM.
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TAS-119 (TAS119) is a potent, selective, orally active inhibitor of Aurora A with IC50 of 1 nM.
TAS-119 displayed high target selectivity among 301 protein kinases, including Aurora B (IC50=95 nM) and Aurora C (IC50=35 nM).
TAS-119 dose dependently enhanced cell growth inhibition by paclitaxel, docetaxel, and cabazitaxel, also potentiated another microtubule stabilizer Epothilone B.
TAS-119 enhanced the antiproliferative effect of paclitaxel in different cell lines, including paclitaxel-resistant cells.
TAS-119 did neither induce mitosis and nor enhance the antiproliferative effect of paclitaxel in normal lung fibroblast cells.
TAS-119 enhanced the antitumor efficacy of paclitaxel and docetaxel in a nude mice NCI-H460 xenograft model, did not exaggerate paclitaxel-induced neutropenia and neurotoxicity.
M.Wt | 506.359 | |
Formula | C23H22Cl2FN5O3 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]- |
1. Sootome H, et al. Mol Cancer Ther. 2020 Oct;19(10):1981-1991.
2. Robbrecht DGJ, et al. Br J Cancer. 2021 Jan;124(2):391-398.
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