Home Cell Cycle PLK inhibitor TAK-960 For research use only.

TAK-960

TAK-960 is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor that has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1).

TAK-960 Chemical Structure

TAK-960 Chemical Structure

CAS: 1137868-52-0

Purity & Quality Control

Batch: S123901 DMSO] 13 mg/mL] false] Ethanol] 3 mg/mL] false] Water] Insoluble] false Purity: 99.92%
99.92

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Biological Activity

Description TAK-960 is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor that has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1).
Features The discovery of TAK -960 provides an interesting example of how the addition of fluorine atoms during optimization significantly alters the attributes of the leads series.
Targets
PLK1 [1]
In vitro
In vitro

TAK-960 has shown activity in several tumor cell lines including those that express multidrug resistant protein 1 (MDR1). [1] Consistent with PLK1 inhibition, TAK-960 treatment gives rise to accumulation of G2/M cells, aberrant "polo" mitosis morphology, and increases phosphorylation of histone H3 (pHH3). [1] TAK-960 inhibits proliferation of multiple cancer cell lines, with mean EC50 values ranging from 8.4 to 46.9 nM, but not in non-dividing normal cells (EC50 >1,000 nM). The mutation status of TP53 or KRAS and MDR1 expression does not correlate with the potency of TAK-960 in the cell lines tested. [1]
Kinase Assay Biochemical kinase inhibition assays
The inhibitory activity of TAK-960 is assessed by the TR-FRET assay, which measures the ATP-dependent phosphorylation of a biotinylated substrate peptide corresponding to residues 2470 through 2488 of the mammalian target of rapamycin protein (Biotin-AGAGTVPESIHSFIGDGLV). A total of 288 kinases are screened for TAK-960 inhibition (1 μM) using HotSpotSM technology and IC50 values for the selected kinases are determined.
Cell Research Cell lines Human tumor cell lines including those with TP53 or KRAS mutations or MDR1 overexpression
Concentrations 0.001-1μM
Incubation Time 72 hours
Method

Cells are seeded into 96-well plates at 3-30 × 103 cells/well in appropriate medium plus 10% fetal calf serum (FCS). After 24 hours, cells are treated with serial dilutions of TAK-960, and 72 hours later, the number of viable cells is assessed using the CellTiter-Glo Assay. Calculation of EC50 values and statistical analysis are done.
In Vivo
In vivo

In animal models, oral administration of TAK-960 increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts. [1] Treatment with once-daily TAK-960 exhibits significant efficacy against multiple tumor xenografts, including an Doxorubicin/Paclitaxel-resistant xenograft model and a disseminated leukemia model. [1]
Animal Research Animal Models Athymic nude mice (BALB/cAJc1-nu/nu), severe combined immunodeficiency (SCID) mice (C.B17-Icr- scid/scid Jcl) or NOD-scid mice (NOD.CB17-Prkdc scid/J)
Dosages 30 mg/kg
Administration Oral dosing
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01179399 Terminated
Advanced Nonhematological Malignancies
Millennium Pharmaceuticals Inc.
 September 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 561.6 Formula

C27H34F3N7O3
CAS No. 1137868-52-0 SDF Download TAK-960 SDF
Smiles COC1=C(NC2=NC=C3N(C)C(=O)C(F)(F)CN(C4CCCC4)C3=N2)C=C(F)C(=C1)C(=O)NC5CCN(C)CC5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 13 mg/mL ( (23.14 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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