Carfilzomib

Catalog # Availability Size / Price Qty
7188/50
7188/10
Carfilzomib | CAS No. 868540-17-4 | Proteasome Inhibitors
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Description: Potent irreversible proteasome inhibitor; active in vivo
Alternative Names: PR-171

Chemical Name:S)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide

Purity: ≥98%

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Biological Activity

Carfilzomib is a potent irreversible proteasome inhibitor. Preferentially inhibits the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50 = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC50 = 14 nM) in vitro with minimal cross-reactivity to other proteases. Exhibits little or no effect on PGPH and T-L activities. Activates prosurvival autophagy and induces cell apoptosis. Acts synergistically with dexamethasone (Cat. No. 1126). Suppresses tumor growth in an in vivo xenograft model. Decreases bone resorption and enhances bone formation in non-tumor bearing mice.

Technical Data

M.Wt:
719.92
Formula:
C40H57N5O7
Solubility:
Soluble to 100 mM in DMSO and to 20 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
868540-17-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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