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PI 3-K inhibitor IX, PIK-90
N-(2,3-Dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide, mTOR Inhibitor VI
A cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC50 = 11, 18, 47, 58, 64, 350, and 830 nM against p110α, p110γ, PI 3-KC2α, p110δ, PI 3-KC2β, p110β, and hsVPS34, respectively), as well as several PIKKs (IC50 = 13, 610, and 1050 nM against DNA-PK, ATM, and mTORC1, respectively) and PI 4-KIIIα (IC50 = 830 nM), while exhibiting much reduced potency against PI 4-KIIIβ and ATR (IC50 = 3.1 and 15 µM, respectively) and little or no activity toward PI 4-KIIα, PIPKs (IC50 >100 µM), and a panel of 36 commonly studied protein kinases (<15% inhibition at 10 µM). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90% at 2.5 µM) and completely prevents insulin-induced blood glucose decline in mice in vivo (10 mg/ml, i.p.).
产品信息
Form Pale yellow solid
Molar mass 351.4
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility DMSO
Chemical formula C18H17N5O3
CAS number 677338-12-4
商店和运输信息
Storage -20°C
Ship Blue Ice Only
Standard Handling |