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528116  PI 3-Kα Inhibitor VIII

N-((1E)-(6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N′-methyl-N′′-(2-methyl-5-nitrobenzene)sulfonohydrazide, HCl

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04 February 2012

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528116-5MG  5 mg 
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A cell-permeable imidazopyridine compound that acts as a highly potent and ATP-competitive DNA-PK and p110α-selective PI3-K inhibitor (IC50 = 0.3, 40, 100, and 850 nM for p110α, p110γ, PI 3-K C2β, and p110β, respectively). Shown to effectively block cellular PI3-K/Akt signaling and inhibit tumor growth both in vitro (IC50 ≤58 nM in MCF7, MCF7 ADR-res, HeLa, A375, and A549 cultures) and in mice in vivo (62% inhibition of HeLa xenograft in 2 weeks, 50 mg/kg/day, i.p.).
Product information
Form Pale yellow solid
Molar mass 524.8
Protect from Light Yes
Hygrocopic Yes
Packaged under inert gas Yes
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C16H14N5O4SBr • HCl • 2H2O
Store and ship information
Storage +2°C to +8°C
Ship Ambient Temperature Only
Regulatory Review
PI 3-Kα Inhibitor VIII, molecular structure

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© Merck KGaA, Darmstadt, Germany, 2012

All references to Merck refer to Merck KGaA, Darmstadt, Germany.

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