A potent

GSK461364 – 25 mg

Brand:
Cayman
CAS:
929095-18-1
Storage:
-20
UN-No:
Non-Hazardous - /

Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} GSK461364 is a potent, reversible inhibitor of Plk1 (Ki = 2.2 nM).{29227} It is less effective against Plk2 and Plk3 (Kis = 860 and 1,000 nM, respectively) and at least 1,000-fold selective for Plk1 over a panel of 48 other kinases.{29227} GSK461364 dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis.{29227} It appears to be more effective against p53-deficient tumors and is able to cross the blood-brain barrier.{29226,29225} GSK461364 is effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice.{29228,29227}  

 

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Description

A potent, reversible, and selective inhibitor of Plk1 (Ki = 2.2 nM); dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis; effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice

Formal name: 5-[6-[(4-methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide

Synonyms:  GSK461364A

Molecular weight: 543.6

CAS: 929095-18-1

Purity: ≥95%

Formulation: A crystalline solid

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

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