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

TAK-960 monohydrochloride 

Cat. No.: HY-15160C
Handling Instructions

TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride 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 monohydrochloride Chemical Structure

TAK-960 monohydrochloride Chemical Structure

CAS No. : 2108449-45-0

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Description

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

In Vitro

TAK-960 monohydrochloride treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 monohydrochloride (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 monohydrochloride (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

598.06

Formula

C₂₇H₃₅ClF₃N₇O₃

CAS No.

2108449-45-0

SMILES

[H]Cl.O=C(NC1CCN(C)CC1)C2=CC(OC)=C(NC3=NC=C(N4C)C(N(C5CCCC5)CC(F)(F)C4=O)=N3)C=C2F

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

TAK-960 monohydrochloridePolo-like Kinase (PLK)proliferationcancercelllinesleukemiamitosisphosphorylationInhibitorinhibitorinhibit

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TAK-960 monohydrochloride
Cat. No.:
HY-15160C
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