In cells

Use at a concentration of 100 nM.

Use the METAP2 inhibitor BAY-896 (biochemical assay human METAP2: IC₅₀ = 39 nM, 2D HUVEC proliferation: IC₅₀ = 390 nM) as additional control. Note: The probe is a racemic mixture.

Use the recommended concentration to avoid off-target toxicity and/or off-target activity. Using concentrations that are higher than recommended could lead to false positive or confounding results.

In vivo

Tested in mice with 5- 25 mg/kg IP for 14 days q2d with good tolerability (body weight); inhibits tumor growth in U87MG and HT1080 Xenograft models in a dose dependent manner; shows fast and potent degradation of METAP2 in mouse lung tissue at 5mg/kg up until at least 48 h post injection.