TAS-119

SKU: orb1695106

Description

TAS-119 is a highly selective, orally bioavailable Aurora A kinase inhibitor (IC50 = 1.0 nM) with significant activity against Aurora B (IC50 = 95 nM). It demonstrates potent antitumor and antimitotic activity in preclinical studies, supporting its investigation in cancer research, including in vivo models of solid tumors.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1453099-83-6
• MW: 506.36
• Purity: 99.65% (May vary between batches)
• Formula: C₂₃H₂₂Cl₂FN₅O₃
• SMILES: Cc1cc(Nc2nc(CC3(CCN(CC3)C(=O)c3cccc(Cl)c3Cl)C(O)=O)ccc2F)n[nH]1
• Target: Aurora Kinase
• Solubility: DMSO:45 mg/mL (88.87 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.95 mM)

Bioactivity

• Target IC50:
  Aurora B:95 nM (IC50)|Aurora A:1 nM (IC50)
• 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.
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• 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.
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Storage & Handling

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

Alternative Names

AuroraKinase, Aurora Kinase, Aurora B, Aurora A, TAS119, TAS-119, TAS 119, TAS 2104, TAS2104, TAS-2104

Compound Identifiers

PubChem CID

71696703