1354799-87-3 (S)-N2-(1-(4-氟苯基)乙基)-4-(1-甲基-1H-吡唑-4-基)-N6-(吡嗪-2-基)吡啶-2,6-二胺 马来酸盐

运输信息：冰袋运输。危险描述：非危险化学品。

Ilginatinib maleate (NS-018 maleate) is a highly effective, oral JAK2 inhibitor with IC50 0.72 nM, selective for JAK2 over JAK1 (46x), JAK3 (54x), Tyk2 (22x). It inhibits Src-family kinases (SRC, FYN) and weakly ABL/FLT3. In vitro, it suppresses JAK2V617F/Mutations cell lines (IC50 11-120 nM) and colony formation in MDS-derived BMMNCs, reducing STAT3 phosphorylation. In vivo, it prolongs survival and reduces splenomegaly in JAK2V617F mouse models at 12.5-100 mg/kg p.o.

生命科学; 医药