TAK-960

SKU: orb1220547

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.(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.TAK-960 (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells.(In Vivo):TAK-960 exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts.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.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1137868-52-0
• MW: 561.6
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₄F₃N₇O₃
• SMILES: COc1cc(C(=O)NC2CCN(C)CC2)c(F)cc1Nc1ncc2N(C)C(=O)C(F)(F)CN(C3CCCC3)c2n1
• Target: PLK
• Solubility: DMSO:35 mg/mL (62.32 mM)

Bioactivity

• In Vivo:
  TAK-960 exhibits (10 mg/kg; p.o. ; once daily for 2 weeks) significant efficacy against multiple tumor xenografts. 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. Animal model: nude mice or SCID mice (bearing HCT116, PC-3, BT474, A549, NCI-H1299, NCI-H1975, A2780, and MV4-11 cells). Dosage: 10 mg/kg. Administration: p.o. ; once daily for 2 weeks. Result: Substantial antitumor activity and good tolerability.
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• 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. TAK-960 (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells. Cell Viability Assay 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PLK