TAK960Oral and selective PLK1 inhibitor CAS# 1137868-52-0 |
- TUG-770
Catalog No.:BCC2018
CAS No.:1402601-82-4
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
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. |
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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. |
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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. |
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.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: |
TAK960 Dilution Calculator
TAK960 Molarity Calculator
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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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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