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Carfilzomib

Chemical Structure : Carfilzomib

CAS No.: 868540-17-4

Carfilzomib (PR 171;PR171;PR-171)

Catalog No.: PC-42598Not For Human Use, Lab Use Only.

Carfilzomib (PR-171) is a potent, highly selective inhibitor chymotrypsin-like activity of proteasome with IC50 of 6 nM.

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Biological Activity

Carfilzomib (PR-171) is a potent, highly selective inhibitor chymotrypsin-like activity of proteasome with IC50 of 6 nM.
Carfilzomib (PR-171) weakly inhibits caspase-like and trypsin-like activities in cellular assays (IC50150-200 nM), also inhibits the chymotrypsin-like activity of the immunoproteasome (IC50=33 nM).
Carfilzomib (PR-171)  accumulates proteasome substrates and induces cell cycle arrest and/or apoptosis.
Carfilzomib (PR-171) shows antitumor efficacy in vivo.

Physicochemical Properties

M.Wt 719.9099
Formula C40H57N5O7
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

L-Phenylalaninamide, (αS)-α-[[2-(4-morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-

References

1. Kuhn DJ, et al. Blood. 2007 Nov 1;110(9):3281-90.

2. Parlati F, et al. Blood. 2009 Oct 15;114(16):3439-47.

3. O'Connor OA, et al. Clin Cancer Res. 2009 Nov 15;15(22):7085-91.

4. Demo SD, et al. Cancer Res. 2007 Jul 1;67(13):6383-91.

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