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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.

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TAK-960, CAS 1137868-52-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 58.00
2 mg	In stock	$ 82.00
5 mg	In stock	$ 123.00
10 mg	In stock	$ 173.00
25 mg	In stock	$ 309.00
50 mg	In stock	$ 515.00
100 mg	In stock	$ 747.00
1 mL * 10 mM (in DMSO)	In stock	$ 173.00

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Purity: 98%

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	PLK3:50.2 nM, PLK1:0.8 nM , PLK2:16.9 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].

Molecular Weight	561.6
Formula	C27H34F3N7O3
CAS No.	1137868-52-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 35 mg/mL (62.32 mM)

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Kinase Inhibitor Library Clinical Compound Library ReFRAME Related Library Bioactive Compound Library Anti-Aging Compound Library

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5-ETHYL-4,5,6,7-TETRAHYDRO-THIAZOLO[5,4-C]PYRIDIN-2-YLAMINE TC-S 7005 3MB-PP1 HMN-214 Mps1-IN-2 Poloxin Pyridoxine Poloxime

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

TAK-960 1137868-52-0 Cell Cycle/Checkpoint PLK Polo-like Kinase (PLK) TAK960 cell TAK 960 cancer proliferation Inhibitor mitosis leukemia inhibit phosphorylation lines inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.