TAK-960

SKU: orb1299985

Description

TAK-960 is a potent, orally active small molecule inhibitor that selectively targets Polo-like kinases (Plks), demonstrating highest potency against Plk1 (IC50 = 0.8 nM). It is a valuable research tool for investigating cell cycle progression and has shown antitumor activity in preclinical cancer models, supporting its use in both in vitro and in vivo studies.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1137868-52-0
• MW: 561.6
• Purity: 98.00% (May vary between batches)
• Formula: C₂₇H₃₄F₃N₇O₃
• SMILES: COc1cc(C(=O)NC2CCN(C)CC2)c(F)cc1Nc1ncc2N(C)C(=O)C(F)(F)CN(C3CCCC3)c2n1
• Target: PLK
• Solubility: DMSO:35 mg/mL (62.32 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.78 mM)

Bioactivity

• Target IC50:
  PLK1:0.8 nM|PLK2:16.9 nM|PTK2/FAK:19.6 nM|FES/FPS:58.2 nM|PLK3:50.2 nM|MLCK/MYLK:25.6 nM
• In Vitro:
  CRC cell lines demonstrated a variable anti-proliferative response to TAK-960 with IC50 values ranging from 0.001 to > 0.75 μmol/L. Anti-proliferative effects were sustained after removal of drug. Following TAK-960 treatment a highly variable accumulation of mitotic (indicating cell cycle arrest) and apoptotic markers was observed. TAK-960 treatment induced G2/M arrest and polyploidy. Six out of the eighteen PDX models responded to single agent TAK-960 therapy (TGII< 20). The addition of TAK-960 to standard of care chemotherapy resulted in largely additive antitumor effects.
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• Cell Research:
  Fifty-five CRC cell lines and 18 PDX models were exposed to TAK-960 and evaluated for proliferation (IC50) and Tumor Growth Inhibition Index, respectively. Additionally, 2 KRAS wild type and 2 KRAS mutant PDX models were treated with TAK-960 as single agent or in combination with cetuximab or irinotecan. TAK-960 mechanism of action was elucidated through immunoblotting and cell cycle analysis.
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Storage & Handling

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

Alternative Names

cancer, cell, Inhibitor, leukemia, lines, inhibit, PLK, mitosis, phosphorylation, Polo-like Kinase (PLK), TAK960, TAK-960, TAK 960, proliferation

Compound Identifiers

PubChem CID

53357478