Bortezomib

Administered via i.v.

U266, IM-9, and Hs Sultan cells

0-10 uM

<=1mg/kg

0.6 nM (Ki) [1], 0.6 nM (Ki) [1], 0.6 nM (Ki) [1], 0.6 nM (Ki) [1], 0.6 nM (Ki) [1], 0.6 nM (Ki) [1]

Bortezomib (0.5 mg/kg and 1.0 mg/kg) causes statistically significant inhibition of tumor growth and a statistically significant prolongation in median overall survival in RPMI8226 xenograft mouse model. [2]

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 uL 10 uL of the stock enzyme solution is added to the cuvette. Reaction progress is monitored by the increase in fluorescence emission at 440 nm (lambdaex = 380 nm) that accompanies cleavage of AMC from peptide-AMC substrates.

384, 24

Data from [Carcinogenesis , 2010, 31, 19481955], Bortezomib (Velcade)purchased from Selleck, (BC) LNCaP (B) and LNCaP-AI (C) cells were transiently transfected with sPLA2-IIa(-800)-Luc (0.5 lg). The cells were then treated with Erlotinib (20 lM), Gefitinib (20 lM), Lapatinib (20 lM), CI-1033 (8 lM), LY294002 (20 lM) and Bortezomib (20 lM) without or with EGF (100 ng/ml) for 24 h. Luciferase assay was performed according to a standard protocol with Renilla luciferase as an internal control. Data are presented as the mean (SD) of duplicate values of a representative experiment that was independently repeated for five times.

DMSO 77 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL