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Bortezomib

Chemical Structure : Bortezomib

CAS No.: 179324-69-7

Bortezomib (PS-341;PS341;PS 341)

Catalog No.: PC-42470Not For Human Use, Lab Use Only.

Bortezomib (PS-341) is a potent, selective, competitive, orally active Proteasome inhibitor with Ki of 0.6 nM for 20S Proteasome.

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Biological Activity

Bortezomib (PS-341) is a potent, selective, competitive, orally active Proteasome inhibitor with Ki of 0.6 nM for 20S Proteasome; shows only modest activity toward serine and thiol proteases (cathepsin G, elastase, chymotrypsin Ki>300 nM); inhibits the TNFα-stimulated activation of NF-κB in primary HUVE cells (IC50=0.5 uM) by blocking the degradation of the inhibitor IκBα; exhibits anti-inflammatory effects in vivo.

Blood Cancer

Approved

Physicochemical Properties

M.Wt 384.2372
Formula C19H25BN4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Boronic acid, B-[(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(2-pyrazinylcarbonyl)amino]propyl]amino]butyl]-

References

1. Palombella VJ, et al. Proc Natl Acad Sci U S A. 1998 Dec 22;95(26):15671-6.

2. Frankel A, et al. Clin Cancer Res. 2000 Sep;6(9):3719-28.

3. Teicher BA, et al. Clin Cancer Res. 1999 Sep;5(9):2638-45.

4. Adams J, et al. Bioorg Med Chem Lett. 1998 Feb 17;8(4):333-8.

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