化合物信息

Description

Solid tumours, Non-small cell lung cancer

Kinetic Methods

In a typical kinetic run, 2.00 mL of assay buffer (20 mM HEPES, 0.5 mM EDTA, 0.035% SDS, pH 7.8) and Suc-Leu-Leu-Val-Tyr-AMC in DMSO are added to a 3 mL fluorescence cuvette, and the cuvette is placed in the jacketed cell holder of a fluorescence spectrophotometer. Reaction temperature is maintained at 37 °C by a circulating water bath. After the reaction solution has reached thermal equilibrium (5 minutes), 1 μL?10 μL of the stock enzyme solution is added to the cuvette. Reaction progress is monitored by the increase in fluorescence emission at 440 nm (λ_ex = 380 nm) that accompanies cleavage of AMC from peptide-AMC substrates.

Cell Lines

U266, IM-9, and Hs Sultan cells

Concentrations

0-10 μM

Incubation Time

48 hours

Methods

Animal Models

Mice are inoculated s.c. into the right flank with RPMI 8226 MM cells.

Formulation

Bortezomib is dissolved in 0.9% sodium chloride.

Doses

≤1mg/kg

Administration

Administered via i.v.