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TAS-119 (TAS-2104) is an orally available, selective and potent inhibitor of Aurora A with an IC50 of 1.0 nM.TAS-119 also inhibits Aurora B with an IC50 of 95 nM.TAS-119 has a higher affinity for Aurora A than for Aurora B.TAS-119 exhibits potent antitumor activity and potential antimitotic activity. TAS-119 has potent anti-tumor activity and potential anti-mitotic activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $98 | In Stock | |
5 mg | $247 | In Stock | |
10 mg | $397 | In Stock | |
25 mg | $788 | In Stock | |
50 mg | $1,230 | In Stock | |
100 mg | $1,730 | In Stock | |
1 mL x 10 mM (in DMSO) | $275 | In Stock |
Description | TAS-119 (TAS-2104) is an orally available, selective and potent inhibitor of Aurora A with an IC50 of 1.0 nM.TAS-119 also inhibits Aurora B with an IC50 of 95 nM.TAS-119 has a higher affinity for Aurora A than for Aurora B.TAS-119 exhibits potent antitumor activity and potential antimitotic activity. TAS-119 has potent anti-tumor activity and potential anti-mitotic activity. |
Targets&IC50 | Aurora A:1 nM (IC50), Aurora B:95 nM (IC50) |
In vitro | TAS-119 (30-300 nM) dose-dependently augments the growth inhibition of HeLa cells induced by three taxanes (Paclitaxel, Docetaxel, and Cabazitaxel). It specifically promotes mitotic accumulation in tumor cells over normal diploid fibroblasts. Moreover, TAS-119 amplifies the antiproliferative efficacy of Paclitaxel across a diverse array of human cancer cell lines, even those resistant to Paclitaxel.[1] |
In vivo | TAS-119 (5, 10, and 30 mg/kg; oral; twice daily on day 1 and every day on day 2; Nude rats injected with HeLa-luc cells) induced pHH3 at all doses in nude rats with the HeLa-luc xenografts. The treatment induces phosphorylated histone H3 (pHH3) in nude rats with the HeLa-luc xenografts.[1] |
Alias | TAS-2104, TAS2104, TAS119, TAS 2104, TAS 119 |
Molecular Weight | 506.36 |
Formula | C23H22Cl2FN5O3 |
Cas No. | 1453099-83-6 |
Smiles | Cc1cc(Nc2nc(CC3(CCN(CC3)C(=O)c3cccc(Cl)c3Cl)C(O)=O)ccc2F)n[nH]1 |
Relative Density. | 1.31g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (88.87 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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