Chemical Name: 2-[5-Methyl-6-(2-methyl-4-pyridinyl)-3-pyridinyl]-N-(5-pyrazin-2-yl-2-pyridinyl)acetamide. Alternate Names: WNT974
Porcupine inhibitor
Molekulargewicht:
396.45
Reinheit:
>98% by HPLC NMR (Conforms)
Formulierung:
Off-white solid
CAS Nummer:
[1243244-14-5]
Formel:
C23H20N6O
Anwendungsbeschreibung:
LGK974 is a potent and selective inhibitor of Porcupine (IC50 = 1 nM). Inhibits Wnt signaling (IC50 = 0.4 nM) in vitro and in vivo.1 It displays efficacy in several cancer models including glioblastoma2,6, squamous cell3, renal cell carcinoma4, and non-small cell lung5. LGK974 reprogrammed the immune suppressive tumor microenvironment in a mouse model of glioblastoma to increase antitumor immune responses.6 It also potentiated anti-PD1 therapy by increasing DC3-like dendritic cells and decreasing myeloid suppressor cells. LGK974 attenuated myocardial ischemia-reperfusion injury by reducing inflammatory responses.7
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