TAK-960 dihydrochloride


Catalog No. Size PriceQuantity
M13827-2 Contact sales@xcessbio.com for quotation $100

Description

TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.

Product information

Molecular Weight: 634.52

Formula: C27H36Cl2F3N7O3

Chemical Name: 4-({9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-5H,6H,7H,8H,9H-pyrimido[4,5-b][1,4]diazepin-2-yl}amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide; bis(chlorohydrogen)

Smiles: Cl.Cl.CN1CCC(CC1)NC(=O)C1=CC(OC)=C(C=C1F)NC1N=C2C(=CN=1)N(C)C(=O)C(F)(F)CN2C1CCCC1

InChiKey: CEMOEYRTQUGSJV-UHFFFAOYSA-N

InChi: InChI=1S/C27H34F3N7O3.2ClH/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);2*1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 3.23 mg/mL (5.09 mM; Need ultrasonic). H2O : 10 mg/mL (15.76 mM; Need ultrasonic).

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 dihydrochloride treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 dihydrochloride (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 dihydrochloride (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells.

In Vivo:

TAK-960 dihydrochloride exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts. In animal models, TAK-960 dihydrochloride (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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