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TAK960Oral and selective PLK1 inhibitor

TAK960

Catalog No. B5860
Size Price Stock Qty
10mM (in 1mL DMSO) $160.00 In stock
5mg $120.00 In stock
10mg $175.00 In stock
50mg $540.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

TAK960

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Chemical Properties

Cas No. 1137868-52-0 SDF Download SDF
Chemical Name 4-((9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide
Canonical SMILES CN1CCC(NC(C2=CC(OC)=C(NC3=NC=C(N(C(C(F)(F)CN4C5CCCC5)=O)C)C4=N3)C=C2F)=O)CC1
Formula C27H34F3N7O3 M.Wt 561.6
Solubility >28.1mg/mL in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

Description:

IC50: 8.4 to 46.9 nmol/L for multiple cancer cell lines

Polo-like kinase 1 (PLK1) is a serine/threonine protein kinase involved in key mitosis processes. Human PLK1 has been shown to be overexpressed in various human cancers. Elevated levels of PLK1 have been associated with poor prognosis, making it an attractive target for anticancer therapy. TAK-960 is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor.

In vitro: TAK-960 treatment caused accumulation of G2–M cells, aberrant polo mitosis morphology, and increased the phosphorylation of histone H3. TAK-960 inhibited proliferation of multiple cancer cell lines, with mean EC50 ranging from 8.4 to 46.9 nmol/L, but not in nondividing normal cells [1].

In vivo: In animal models, oral administration of TAK-960 increased pHH3 in a dose-dependent manner and significantly inhibited the growth of HT-29 colorectal cancer xenografts. Once daily treatment TAK-960 exhibited significant efficacy against multiple tumor xenografts, including an adriamycin/paclitaxel-resistant xenograft model and a disseminated leukemia model [1].

Clinical trial: TAK-960 is currently undergoing Phase I evaluation in adult patients with advanced non-hematologic malignancies.

Reference:
[1] Hikichi Y, Honda K, Hikami K, Miyashita H, Kaieda I, Murai S, Uchiyama N, Hasegawa M, Kawamoto T, Sato T, Ichikawa T, Cao S, Nie Z, Zhang L, Yang J, Kuida K, Kupperman E.  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.
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