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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Cell Cycle >PLK inhibitors >GSK461364

GSK461364

GSK461364 Structure
  • ₹0
  • Product name: GSK461364
  • CAS: 929095-18-1
  • MF: C27H28F3N5O2S
  • MW: 543.6
  • EINECS:200-258-5
  • MDL Number:MFCD12755419
  • Synonyms:(R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide;GSK-461364A;GSK461364(GSK-461364);5-[6-[(4-Methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl];5-[6-[(4-Methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phen;GSK461364;GSK-461364;GSK4613
Manufacturer Product number Product description Packaging Price Updated Buy

Properties

Melting point :>150°C (dec.)
Boiling point :658.0±65.0 °C(Predicted)
Density :1.39
storage temp. :Hygroscopic, -20°C Freezer, Under inert atmosphere
solubility :Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
pka :15.16±0.50(Predicted)
form :Solid
color :Off-White to Light Beige

Safety Information

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Description

Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. GSK461364 is a potent, reversible inhibitor of Plk1 (Ki = 2.2 nM). 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. GSK461364 dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis. It appears to be more effective against p53-deficient tumors and is able to cross the blood-brain barrier. GSK461364 is effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice.

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