| Name | TAK-960 |
| Description | TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively. |
| 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[1]. |
| 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 |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 35 mg/mL (62.32 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.78 mM), Sonication is recommended.
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| Keywords | TAK-960 | TAK960 | TAK 960 | proliferation | Polo-like Kinase (PLK) | PLK | phosphorylation | mitosis | lines | leukemia | Inhibitor | inhibit | cell | cancer |
| Inhibitors Related | T521 | (E/Z)-Rigosertib sodium | Cyclapolin 9 | SBE13 Hydrochloride | Pyridoxine | Rigosertib sodium | 3MB-PP1 | Ro3280 | Volasertib | Poloxin-2 | BI 2536 | GSK461364 |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Cell Cycle Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
