Formulation: A solid
Formal Name: 3-[(4R)-7-chloro-10-[3-(4-chloro-3,5-dimethylphenoxy)propyl]-3,4-dihydro-4-methyl-1-oxo-6-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyrazino[1,2-a]indol-2(1H)-yl]-1-methyl-1H-indole-5-carboxylic acid
Purity: ≥98%
Formula Markup: C39H39Cl2N5O4
Formula Weight: 712,7
Shelf life (days): 1460
CAS Number: 2131184-57-9
Notes: 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}
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