产品描述:
VU0661013 is an inhibitor of myeloid cell leukemia-1 (Mcl-1; Ki = 97 pM).{72138} It is selective for Mcl-1 over Bcl-xL and Bcl-2 (Kis = >40 and 0.73 µM, respectively). VU0661013 inhibits cell growth in a panel of acute myeloid leukemia (AML) cell lines (GI50s = 0.16-7.62 µM). It decreases blood, bone marrow, and spleen leukemic burden, reduces splenomegaly, and increases survival in a MV4-11 disseminated AML mouse xenograft model when administered at a dose of 75 mg/kg. VU0661013 also selectively inhibits glutathione peroxidase 4 (GPX4; IC50 = 8.4 µM) over GPX1, GPX2, glutathione reductase (GR), and thioredoxin reductase 1 (TrxR1).{72139}