Vevorisertib (ARQ 751) is an orally active allosteric AKT inhibitor that blocks AKT phosphorylation. Vevorisertib inhibits tumor cell proliferation through Cyclin D1 and Ki67. Vevorisertib inhibits liver fibrosis through collagen accumulation, alpha-SMA, COL1, and TGF-beta. Vevorisertib reduces total bilirubin. Vevorisertib significantly reduces tumor size in a cirrhotic rat HCC model. Vevorisertib can be used for research on hepatocellular carcinoma [1].
In Vivo, Vevorisertib (10 mg/kg/day; p.o.; daily; 15 days) significantly reduces tumor size, decreases tumor number, inhibits tumor cell proliferation, and ameliorates liver fibrosis in the diethylnitrosamine (DEN)-induced cirrhotic rat HCC model[1].
In Vitro, Vevorisertib completely blocks AKT (Ser473) phosphorylation in Hep3B, HepG2, HuH7, and PLC/PRF/5 cell lines at both IC20 and IC50 concentrations[1].
References:
[1]. Kurma K, et al. Effect of Novel AKT Inhibitor Vevorisertib as Single Agent and in Combination with Sorafenib on Hepatocellular Carcinoma in a Cirrhotic Rat Model. International journal of molecular sciences. 2022 Dec 19;23(24):16206.
In Vivo, Vevorisertib (10 mg/kg/day; p.o.; daily; 15 days) significantly reduces tumor size, decreases tumor number, inhibits tumor cell proliferation, and ameliorates liver fibrosis in the diethylnitrosamine (DEN)-induced cirrhotic rat HCC model[1].
In Vitro, Vevorisertib completely blocks AKT (Ser473) phosphorylation in Hep3B, HepG2, HuH7, and PLC/PRF/5 cell lines at both IC20 and IC50 concentrations[1].
References:
[1]. Kurma K, et al. Effect of Novel AKT Inhibitor Vevorisertib as Single Agent and in Combination with Sorafenib on Hepatocellular Carcinoma in a Cirrhotic Rat Model. International journal of molecular sciences. 2022 Dec 19;23(24):16206.