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TAK-960

Catalog No. T7200Cas No. 1137868-52-0

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.

TAK-960

TAK-960

Purity: 97.06%
Catalog No. T7200Cas No. 1137868-52-0
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.
Pack SizePriceAvailabilityQuantity
1 mg$58In Stock
2 mg$82In Stock
5 mg$123In Stock
10 mg$173In Stock
25 mg$309In Stock
50 mg$515In Stock
100 mg$747In Stock
1 mL x 10 mM (in DMSO)$173In Stock
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Purity:97.06%
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Product Introduction

Bioactivity
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.
Targets&IC50
PLK1:0.8 nM , PLK2:16.9 nM , PLK3:50.2 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
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].
Chemical Properties
Molecular Weight561.6
FormulaC27H34F3N7O3
Cas No.1137868-52-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 35 mg/mL (62.32 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7806 mL8.9031 mL17.8063 mL89.0313 mL
5 mM0.3561 mL1.7806 mL3.5613 mL17.8063 mL
10 mM0.1781 mL0.8903 mL1.7806 mL8.9031 mL
20 mM0.0890 mL0.4452 mL0.8903 mL4.4516 mL
50 mM0.0356 mL0.1781 mL0.3561 mL1.7806 mL

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