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TAS-119

Chemical Structure : TAS-119

CAS No.: 1453099-83-6

TAS-119 (TAS119)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 506.359
Formula C23H22Cl2FN5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]-

References

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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