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Bortezomib

Bortezomib

Item no.	S1013-25
Manufacturer	Selleckchem
CASRN	179324-69-7
Amount	25 mg
Quantity options	100 mg 1 g 10 g 10 mM/1 mL 25 mg 300 mg 5 mg 5 g
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Lymphatic System Cancer
Type	Inhibitors
Specific against	other
Smiles	B(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	LDP-341,MLM341,NSC 681239,PS-341
Similar products	Bortezomib
Available
Storage Conditions	3 years -20°C (in the dark) powder 1 year -80°C (in the dark) in solvent
Molecular Weight	384, 24
Administration	Administered via i.v.
Animal Models	Mice are inoculated s.c. into the right flank with RPMI 8226 MM cells.
Cell lines	U266, IM-9, and Hs Sultan cells
Clinical Trials	Bortezomib is currently in Phase I/II clinical trials in patients with Non-small Cell Lung Cancer.
Concentrations	0-10 uM
Dosages	<=1mg/kg
Formulation	Bortezomib is dissolved in 0.9% sodium chloride.
IC50	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]
In vitro	Bortezomib has significant inhibitory effect on the growth of multiple myeloma (MM) cell lines including U266, IM-9, and Hs Sultan with IC50 of 3 nM, 6 nM and 20 nM, respectively. Proliferation of RPMI8226 MM cells resistant to conventional therapies are also inhibited by Bortezomib with IC50 of 30 nM, 40 nM, 20 nM and 20 nM for RPMI8226, Dox40, MR20, and LR5 cells, respectively. Furthermore, Bortezomib effectively inhibits the growth of four patients' MM cells (MM1â€“4) with IC50 of 3.5 nM, 5 nM, 30 nM, and 2.5 nM, respectively. [1]
In vivo	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]
Incubation Time	48 hours
Kinase Assay	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.
Method	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 L of 5 mg/mL MTT to each well for the last 4 hour of 48-hour cultures, followed by 100 L of isopropanol containing 0.04 N HCl. Absorbance is measured at 570 nm using a spectrophotometer.
Solubility (25C)	DMSO 77 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	Bortezomib is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.

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S1013-25-datasheet.pdf

S1013-25-safety-datasheet.pdf