TAK960

Oral and selective PLK1 inhibitor CAS# 1137868-52-0

TAK960

2D Structure

Catalog No. BCC6411----Order now to get a substantial discount!

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Quality Control of TAK960

Quality Control & MSDS

3D structure

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TAK960

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Chemical Properties of TAK960

Cas No. 1137868-52-0 SDF Download SDF
PubChem ID 53357478 Appearance Powder
Formula C27H34F3N7O3 M.Wt 561.6
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 35 mg/mL (62.32 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-8H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide
SMILES CN1CCC(CC1)NC(=O)C2=CC(=C(C=C2F)NC3=NC=C4C(=N3)N(CC(C(=O)N4C)(F)F)C5CCCC5)OC
Standard InChIKey GWRSATNRNFYMDI-UHFFFAOYSA-N
Standard InChI InChI=1S/C27H34F3N7O3/c1-35-10-8-16(9-11-35)32-24(38)18-12-22(40-3)20(13-19(18)28)33-26-31-14-21-23(34-26)37(17-6-4-5-7-17)15-27(29,30)25(39)36(21)2/h12-14,16-17H,4-11,15H2,1-3H3,(H,32,38)(H,31,33,34)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of TAK960

DescriptionTAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively.In Vitro:TAK-960 inhibits full-length PLK1 protein with IC50 of 0.8 nM, wich is 20-fold lower than the next lowest IC50 value (PLK2: 16.9 nM). TAK-960 (2-1000 nM) causes accumulation of G2-M cells in HT-29 cells. TAK-960 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. TAK-960 does not sensitize cancer cells to radiation when an insufficient amount of time is provided to induce mitotic arrest. The overexpression of a PLK1 mutant, PLK1-R136G&T210D;, which is confirmed to cancel the TAK-960-mediated increase in the proportion of mitotic cells, abrogates the radiosensitizing effects of TAK-960[2].In Vivo:TAK-960 (7.5 mg/kg, p.o.) shows a significant increase in median survival compared with vehicle in MV4-11 human leukemia model. TAK-960 (10 mg/kg, p.o.) inhibits tumor growth in the MDR1-expressing K562ADR-bearing leukemia xenograft model[1]. TAK-960 (10 mg/kg) significantly suppresses tumor growth when combined with IR in tumor xenografts[2].

References:
[1]. Hikichi Y, et al. 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. [2]. Inoue M, et al. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27;5:15666.

Protocol

Kinase Assay [1]
The inhibitory activity of TAK-960 is assessed by the TR-FRET (fluorescence resonance energy transfer) assay, which measures the ATP-dependent phosphorylation of a biotinylated substrate peptide corresponding to residues 2,470 through 2,488 of the mTOR protein (Biotin-AGAGTVPESIHSFIGDGLV). A total of 288 kinases are screened for TAK-960 inhibition (1 μM) using HotSpot technology and IC50 values for the selected kinases are determined.

Cell Assay [1]
Cells are seeded into 96-well plates at 3,000 to 30,000 cells per well in appropriate medium plus 10% fetal calf serum. 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 using GraphPad Prism software.

Animal Administration [2]
The suspension of HeLa cells (2×106 in 100 μL PBS) or H1299 cells (3×106 in 100 μL PBS) is subcutaneously inoculated into the right hind legs of 8-week-old nude mice (BALB/c nu/nu mice). The indicated dose of TAK-960 is orally administered to tumor-bearing mice. In the radiation treatment, tumor xenografts are locally irradiated with the indicated dose of 137Cs γ-rays using a Gammacell 40 Exactor.

References:
[1]. Hikichi Y, et al. 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. [2]. Inoue M, et al. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27;5:15666.

TAK960 Dilution Calculator

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TAK960 Molarity Calculator

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Preparing Stock Solutions of TAK960

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.7806 mL 8.9031 mL 17.8063 mL 35.6125 mL 44.5157 mL
5 mM 0.3561 mL 1.7806 mL 3.5613 mL 7.1225 mL 8.9031 mL
10 mM 0.1781 mL 0.8903 mL 1.7806 mL 3.5613 mL 4.4516 mL
50 mM 0.0356 mL 0.1781 mL 0.3561 mL 0.7123 mL 0.8903 mL
100 mM 0.0178 mL 0.089 mL 0.1781 mL 0.3561 mL 0.4452 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on TAK960

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.
[2]
[3]

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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 at 10 μM ATP; TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively.

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