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Tocris/TAK 960 hydrochloride/5403/10/10 mg

价格: ¥3060.00 市场价: 5100.00

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货号: 5403/10

品牌: Tocris

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Description: Potent and selective PLK1 inhibitor

Chemical Name: 4-[(9-Cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methyl-4-piperidinyl)benzamide hydrochloride

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent PLK1 inhibitor (IC₅₀ values are 0.8, 16.9 and 50.2 nM for PLK1, PLK2 and PLK3 respectively). Exhibits >20-fold selectivity for PLK1 over FAK, MLCK and FES, and has minimal activity against a panel of 282 other kinases. Inhibits proliferation of a range of cancer cell lines in vitro and inhibits tumor growth of multiple human cancer cell xenografts in vivo. Orally bioavailable.

Compound Libraries

TAK 960 hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	598.06
Formula	C₂₇H₃₄F₃N₇O₃.HCl
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1137868-96-2
PubChem ID	91826087
InChI Key	QZBHDFGFNVMONB-UHFFFAOYSA-N
Smiles	O=C1C(F)(F)CN(C3CCCC3)C(N=C(NC4=CC(F)=C(C(NC5CCN(C)CC5)=O)C=C4OC)N=C2)=C2N1C.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	59.81	100

Preparing Stock Solutions

The following data is based on the product molecular weight 598.06. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.67 mL	8.36 mL	16.72 mL
5 mM	0.33 mL	1.67 mL	3.34 mL
10 mM	0.17 mL	0.84 mL	1.67 mL
50 mM	0.03 mL	0.17 mL	0.33 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Hikichi et al (2012) 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. 11 700 PMID: 22188812

Nie et al (2013) Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1). Bioorg.Med.Chem.Lett. 23 3662 PMID: 23664874

Keywords: TAK 960 hydrochloride, supplier, TAK960, hydrochloride, potent, PLK1, inhibitors, inhibits, selective, orally, bioavailable, antitumor, 1137868520, Polo-like, Kinase, Mitosis, Polo-like, Kinase, Tocris Bioscience

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