GSK-2269557

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK-2269557 是一种高效、选择性的 PI3Kδ 抑制剂 (pKi=9.9)。

GSK-2269557 is a highly potent and selective inhibitor of PI3Kδ (pKi=9.9); displays >1000 fold selectivity versus other PI3K isoforms; inhibits both IFNγ and IL-2 production in a concentration-dependent manner, with pIC50 values of 8.2 and 8.1, respectively, in a human lung parenchyma assay; shows activity in rat acute OVA model of Th2-driven lung inflammation (ED50=67ug/kg).COPD Phase 2 Clinical.

Nemiralisib (GSK2269557 free base) is highly selective for PI3Kδ, with >1000-fold selectivity over the closely related isoforms PI3Kα (pIC50=5.3), PI3Kβ (pIC50=5.8) and PI3Kγ (pIC50=5.2). Nemiralisib inhibits IFNγ in the peripheral blood mononuclear (PBMC) assay with an pIC50 of 9.7.

To assess the suitability of the series for inhaled delivery clearance data in rat microsomes and subsequently in vivo pharmacokinetic data from Sprague Dawley male rats is obtained. Compounds (e.g., Nemiralisib) are administered by the oral or intravenous routes, at a dose level of 3 and 1mg/kg respectively (n=2 rats/route). Nemiralisib free base is active in a disease relevant brown norway rat acute OVA model of Type 2 helper T-cells (Th2)-driven lung inflammation.

GSK2269557 | Nemiralisib

PI3K/Akt/mTOR signaling

PI3K

PI3K

Inflammation/Immunology

COPD

1254036-71-9

440.5401

C26H28N6O

>98% (HPLC)

DMSO: ≥ 31 mg/mL

CC(N1CCN(CC2=CN=C(C3=CC(C4=CC=CC5=C4C=CN5)=CC6=C3C=NN6)O2)CC1)C

1H-Indazole, 6-(1H-indol-4-yl)-4-[5-[[4-(1-methylethyl)-1-piperazinyl]methyl]-2-oxazolyl]-

(-20℃)

With Ice Pack

≥ 2 years