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

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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
Product Name:4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]-
Synonyms:4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]-;TAS 2104;TAS2104;TAS-2104;VIC-1911 (TAS-119);TAS119|||TAS2104|||TAS 2104|||TAS-2104|||TAS 119;TAS-119, 10 mM in DMSO;TAS-119
CAS:1453099-83-6
MF:C23H22Cl2FN5O3
MW:506.36
EINECS:
Product Categories:APIs
Mol File:1453099-83-6.mol
4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]- Structure
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
Safety Information
MSDS Information
4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]- Usage And Synthesis
UsesTAS-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 50Aurora 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
Tag:4-Piperidinecarboxylic acid, 1-(2,3-dichlorobenzoyl)-4-[[5-fluoro-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyridinyl]methyl]-(1453099-83-6) Related Product Information
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