tcsc0474 Galunisertib

Galunisertib (LY2157299) is a selective TGF-β receptor inhibitor with an IC₅₀ of 56 nM.

IC50 & Target: IC50: 56 nM (TGF-βR)^[1]

In Vitro: Galunisertib (LY2157299) is a selective ATP-mimetic inhibitor of TGF-β receptor (TβR)-I activation LY2157299 (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Sorafenib in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines^[2].

In Vivo: Human xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) are implanted subcutaneously in nude mice. After oral administration of 75 mg/kg, Galunisertib (LY2157299) induces a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline is approximately 6 h after administration^[3].