1. Cell Cycle/DNA Damage
  2. Polo-like Kinase (PLK)
  3. TAK-960

TAK-960 

Cat. No.: HY-15160 Purity: 97.59%
Handling Instructions

TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.

For research use only. We do not sell to patients.

TAK-960 Chemical Structure

TAK-960 Chemical Structure

CAS No. : 1137868-52-0

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5 mg USD 156 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 648 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1008 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts[1].

IC50 & Target[1]

PLK1

0.8 nM (IC50)

PLK2

16.9 nM (IC50)

PLK3

50.2 nM (IC50)

FAK/PTK2

19.6 nM (IC50)

MLCK/MYLK

25.6 nM (IC50)

FES/FPS

58.2 nM (IC50)

In Vitro

TAK-960 treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines, with mean EC50 values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells[1].
TAK-960 (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells[2].

Cell Viability Assay[1]

Cell Line: HT-29, HCT116, COLO320DM, HCT-15, RKO, SW480, K-562….Hela, DU 145 cells
Concentration: 2-1000 nM
Incubation Time: 72 hours
Result: Inhibited proliferation of human cancer cell lines regardless of TP53 and KRAS mutation and MDR1 expression status.
In Vivo

TAK-960 exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts[1].
In animal models, TAK-960 (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts[1].

Animal Model: nude mice or SCID mice (bearing HCT116, PC-3, BT474, A549, NCI-H1299, NCI-H1975, A2780, and MV4-11 cells)[1]
Dosage: 10 mg/kg
Administration: P.o.; once daily for 2 weeks
Result: Substantial antitumor activity and good tolerability.
Clinical Trial
Molecular Weight

561.60

Formula

C₂₇H₃₄F₃N₇O₃

CAS No.

1137868-52-0

SMILES

O=C(NC1CCN(C)CC1)C2=CC(OC)=C(NC3=NC=C(N4C)C(N(C5CCCC5)CC(F)(F)C4=O)=N3)C=C2F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (3.56 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7806 mL 8.9031 mL 17.8063 mL
5 mM --- --- ---
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

TAK-960TAK960TAK 960Polo-like Kinase (PLK)proliferationcancercelllinesleukemiamitosisphosphorylationInhibitorinhibitorinhibit

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Product Name:
TAK-960
Cat. No.:
HY-15160
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