物质信息

ID:73025

名称和标识
IUPAC传统名
@bortezomib
IUPAC标准名
[(1R)-3-methyl-1-[(2S)-3-phenyl-2-(pyrazin-2-ylformamido)propanamido]butyl]boronic acid
别名
VelcadeMG-341PS-341Bortezomib
数据登录号
化合物性质
药理学性质
作用靶点
IGF-1R
理化性质
溶解度
DMSO
安全信息
保存条件
-20°C
产品相关信息
成盐信息
Free Base
描述信息
Research Area
Description
Solid tumours, Non-small cell lung cancer
Protocol
Kinase Assay [1]
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 (λex = 380 nm) that accompanies cleavage of AMC from peptide-AMC substrates.
Cell Assay [1]
Cell Lines
U266, IM-9, and Hs Sultan cells
Concentrations
0-10 μM
Incubation Time
48 hours
Methods

The inhibitory effect of Bortezomib on MM and BMSC growth is assessed by measuring MTT dye absorbance of the cells. Cells from 48-hour cultures are pulsed with 10 μL of 5 mg/mL MTT to each well for the last 4 hour of 48-hour cultures, followed by 100 μL of isopropanol containing 0.04 N HCl. Absorbance is measured at 570 nm using a spectrophotometer.

Animal Study [2]
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.
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参考文献
• Nie D, et al. Leuk Lymphoma, 2012.
• Yu C, et al. Blood, 2003, 102(10), 3765-3774.
• Hideshima T, et al. Cancer Res, 2001, 61(7), 3071-3076.
• LeBlanc R, et al. Cancer Res, 2002, 62(17), 4996-5000.