Aktywny doustnie inhibitor multikinazy najlepiej znany ze swojej aktywności ALK4, receptorów TGFbeta TGFβ-RI (ALK5) i TGFβ-RII oraz skuteczności przeciwnowotworowej in vitro i in vivo.
Galunisertib (LY2157299) jest aktywnym doustnie inhibitorem multikinazy (IC50 w nM = 80/ALK4, 170/TGFβR1, 210/TGβ?R2, 190/MINK (MAP4K6), 220/RIP2 (RIPK2), 260/CK1α, 280/MEKK4, 310/GAK, 400/CK1ε, 470/ALK6 (BMPR1B), 500/B-raf, 510/TNIK) cytowany głównie ze względu na ALK4 & Receptory TGFbeta (TGFβ) (TGFβ-RI (ALK5) i TGFβ-RII) aktywność hamująca i skuteczność przeciwnowotworowa in vitro (0.1-10 μM) i in vivo (20-100 mg/kg p.o.; myszy).
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