Description
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
Product information
CAS Number: 1137868-96-2
Molecular Weight: 598.06
Formula: C27H35ClF3N7O3
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;hydrochloride
Smiles: Cl.CN1CCC(CC1)NC(=O)C1=CC(OC)=C(C=C1F)NC1=NC2=C(C=N1)N(C)C(=O)C(F)(F)CN2C1CCCC1
InChiKey: QZBHDFGFNVMONB-UHFFFAOYSA-N
InChi: InChI=1S/C27H34F3N7O3.ClH/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);1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
TAK-960 hydrochloride treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 hydrochloride (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 hydrochloride (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells.
In Vivo:
TAK-960 hydrochloride exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts. In animal models, TAK-960 hydrochloride (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts.
Products are for research use only. Not for human use.
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