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Cell Cycle/Checkpoint PLK TAK-960

TAK-960

Catalog No. T7200   CAS 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, CAS 1137868-52-0
Pack Size Availability Price/USD Quantity
2 mg In stock 92.00
5 mg In stock 138.00
10 mg In stock 193.00
25 mg In stock 344.00
50 mg In stock 573.00
100 mg In stock 899.00
1 mL * 10 mM (in DMSO) In stock 203.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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 : ic50 0.8 nM,   Plk2 : ic50 16.9 nM,   Plk3 : ic50 50.2 nM,  
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].
Molecular Weight 561.6
Formula C27H34F3N7O3
CAS No. 1137868-52-0

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 35 mg/mL (62.32 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Klauck P J , Bagby S M , Capasso A , et al. Antitumor activity of the polo-like kinase inhibitor, TAK-960, against preclinical models of colorectal cancer[J]. BMC Cancer, 2018, 18(1):136. 2. Hikichi Y, Honda K, Hikami K,et al.TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens[J].Mol Cancer Ther. 2012 Mar;11(3):700-9. 3. Nie Z , Feher V , Natala S , et al. Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1).[J]. Bioorganic & Medicinal Chemistry Letters, 2013, 23(12):3662-3666.

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