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Product Details

Carfilzomib | Proteasome inhibitor

Carfilzomib (868540-17-4) is a potent and irreversible proteasome inhibitor.1 Synthetic analog of the microbial product epoxomcin.2 Compared to bortezomib it displays equal potency but greater selectivity for the chymotrypsin-like activity of the proteasome. In cell culture it is more cytotoxic than bortezomib and hematologic tumor cells exhibit greater sensitivity than solid tumor cells. Treatment of cells with carfilzomib results in the accumulation of proteasome substrates and induction of cell cycle arrest and/or apoptosis.3 Effective against multiple myeloma.4 Active in vivo.

References/Citations
1) Bennett and Kirk (2008) Development of proteasome inhibitors in oncology and autoimmune diseases; Curr. Opin. Drug Disc. Dev. 11 616
2) Hanada et al. (1992), Epoxomicin, a new antitumor agent of microbial origin; J. Antibiot. (Tokyo), 45 174
3) Demo et al. (2007) Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome; Cancer Res. 67 6383
4) Kuhn et al. (2007), Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma; Blood, 110 328

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Carfilzomib | 868540-17-4 | Structure | supplier

Catalog#  10-1477

$50.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
868540-17-4
Catalog Number:
10-1477
Activity:
Proteasome inhibitor
Alternate Names:
PR-171
Chemical Name:
(αS)-α-[[2-(4-morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]- L-Phenylalaninamide
Molecular Weight:
719.93
Molecular Formula:
C40H57N5O7
Solubility:
Soluble in DMSO (up to 80 mg/ml) or in Ethanol (up to 25 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 week.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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