GSK461364A

GSK461364A

Biochem/physiol Actions

GSK461364 is an imidazotriazine derivate that inhibits polo-like kinase 1 (Plk1) in a potent, reversible, ATP-competitive, and highly selective manner (Kiapp ﹤0.5 nM vs. 0.86 µM for Plk2 and 200 µM for Plk3; ATP Kmapp = 16 µM), exhibiting much reduced or little potency toward a panel of 262 kinases. GSK461364A inhibits the growth of various cancer cultures (IG50 ﹤100 nM) as a result of either growth arrest (cytostasis) or cytotoxicity in vitro and effectively suppresses the expansion of various human tumor exnografts in mice in vivo (25 or 50 mg/kg i.p. q2dx12).

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Code Description Colour Quality Level Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575539 GSK461364A white to beige 100 SIGMA-ALDRICH 2-8°C
£491.68 (exc VAT) per 25MG
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3575540 GSK461364A white to beige 100 SIGMA-ALDRICH 2-8°C
£151.82 (exc VAT) per 5MG
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