Home Tools

TAK-960 monohydrochloride

Catalog No. T39553 CAS 2108449-45-0

TAK-960 monohydrochloride is an orally available compound that selectively inhibits polo-like kinase 1 (PLK1) with an IC 50 of 0.8 nM. It also demonstrates inhibitory activity against PLK2 (IC 50 of 16.9 nM) and PLK3 (IC 50 of 50.2 nM). Moreover, TAK-960 monohydrochloride effectively suppresses the proliferation of various cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.

All TargetMol products are for research or drug registration purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose in violation of laws and regulations.

TAK-960 monohydrochloride Chemical Structure

TAK-960 monohydrochloride, CAS 2108449-45-0

Pack Size	Availability	Price/USD	Quantity
10 mg	35 days	$ 825.00
50 mg	35 days	$ 3,450.00

Bulk Inquiry

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TAK-960 monohydrochloride is an orally available compound that selectively inhibits polo-like kinase 1 (PLK1) with an IC 50 of 0.8 nM. It also demonstrates inhibitory activity against PLK2 (IC 50 of 16.9 nM) and PLK3 (IC 50 of 50.2 nM). Moreover, TAK-960 monohydrochloride effectively suppresses the proliferation of various cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
In vitro	Treatment with TAK-960 monohydrochloride induces G2-M cell accumulation, abnormal polo-like kinase mitosis morphology, and elevates histone H3 phosphorylation (pHH3). At concentrations ranging from 2-1000 nM over 72 hours, TAK-960 monohydrochloride effectively suppresses the proliferation of a broad spectrum of cancer cell lines, exhibiting mean EC 50 values between 8.4 and 46.9 nM, while sparing nondividing normal cells[1]. Specifically, an 8 nM concentration of TAK-960 monohydrochloride results in G2/M cell cycle arrest, demonstrating minimal cytotoxicity in HeLa cells[2]. This inhibition includes cells regardless of TP53 and KRAS mutation status, as well as MDR1 expression, highlighting its potential broad applicability in cancer treatment.
In vivo	TAK-960 monohydrochloride, administered orally at a dosage of 10 mg/kg once daily for two weeks, has demonstrated significant efficacy in treating multiple tumor xenografts, including those in nude or SCID mice implanted with a variety of cancer cells such as HCT116, PC-3, BT474, A549, NCI-H1299, NCI-H1975, A2780, and MV4-11. This compound notably increases pHH3 levels in a dose-dependent manner and has shown considerable effectiveness in inhibiting the growth of HT-29 colorectal cancer xenografts, exhibiting both substantial antitumor activity and good tolerability in these models.

Molecular Weight	598.07
Formula	C27H35ClF3N7O3
CAS No.	2108449-45-0

Storage

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

References and Literature

1. Hikichi Y, 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. Mol Cancer Ther. 2012 Mar;11(3):700-9. 2. Inoue M, et al. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27;5:15666.

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

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 monohydrochloride 2108449-45-0 TAK 960 Monohydrochloride TAK960 Monohydrochloride TAK960 monohydrochloride TAK960 TAK 960 TAK-960 Monohydrochloride TAK 960 monohydrochloride TAK-960 inhibitor inhibit

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