TAS-119

SKU: orb2901100

Description

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.

Key Properties

• CAS Number: 1453099-83-6
• MW: 506.36
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₂Cl₂FN₅O₃
• SMILES: Cc1cc(Nc2nc(CC3(CCN(CC3)C(=O)c3cccc(Cl)c3Cl)C(O)=O)ccc2F)n[nH]1
• Target: Aurora Kinase
• Solubility: In Vitro: DMSO : 50 mg/mL (98.74 mM; Ultrasonic )

Bioactivity

• 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. Animal model: Nude rats injected with HeLa-luc cells. 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.
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• In Vitro:
  TAS-119 enhances the antiproliferative effect of Paclitaxel in a variety of human cancer cell lines, including Paclitaxel-resistant cells. TAS-119 (30-300 nM) dose dependently enhances cell growth inhibition by three taxanes (Paclitaxel, Docetaxel, and Cabazitaxel) in HeLa cells. TAS-119 induces mitotic accumulation predominantly in tumor cells, compared with that in normal diploid fibroblasts.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Aurora Kinase