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| | 4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]- Basic information |
| | 4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]- Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO : 50 mg/mL (98.74 mM; Need ultrasonic) | | form | Solid | | color | White to off-white |
| | 4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]- Usage And Synthesis |
| Uses | 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]. | | in vivo | 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]. | Animal Model: | Nude rats injected with HeLa-luc cells[1] | | Dosage: | 5 mg/kg, 10 mg/kg, and 30 mg/kg | | Administration: | Oral administration; twice daily on day 1 and everyday on day 2 | | Result: | Induced pHH3 at all doses in nude rats with the HeLa-luc xenografts. |
| | IC 50 | Aurora A: 1 nM (IC50); Aurora B: 95 nM (IC50) | | References | [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. DOI:10.1158/1535-7163.MCT-20-0036 |
| | 4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]- Preparation Products And Raw materials |
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