GSK461364

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GSK461364

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Cat No: 18099

Biochemicals - Kinase Inhibitors

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...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

1000873-97-1 biochemical inhibitor protein kinase intracellular signaling cell cycle cancer inhibit GSK 461364 461364A GSK461364-A Plk-1 reversible polo-like Plk1

Product Overview:
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}

Size	1 mg
Shipping	dry ice
CAS Number	929095-18-1
Molecular Formula	C₂₇H₂₈F₃N₅O₂S
SMILES	CN1CCN(CC1)CC2=CC3=C(C=C2)N=CN3C4=CC(O[C@H](C)C5=C(C(F)(F)F)C=CC=C5)=C(S4)C(N)=O
Molecular Weight	543,6
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2933.59
UNSPSC code	12352100

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MSDS

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