A selective inhibitor of Plks (IC50s = 0.8

TAK-960 – 5 mg

Brand:
Cayman
CAS:
1137868-52-0
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively.{31040,31041} It exhibits greater than 20-fold selectivity for Plk1 over FAK, MLCK, and the tyrosine protein kinase Fes, and has minimal activity against a panel of 282 other kinases.{31040,31041} It inhibits the proliferation of various cancer cell lines, including MDR1-expressing tumors, and also prevents tumor growth in several human cancer cell xenograft models, including a disseminated model of AML- and MDR1-expressing hematological tumors.{31040,31041}  

 

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Description

A selective inhibitor of Plks (IC50s = 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively); inhibits the proliferation of various cancer cell lines and prevents tumor growth in several human cancer cell xenograft models

Formal 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

Synonyms: 

Molecular weight: 561.6

CAS: 1137868-52-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Plks||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PLK Signaling

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