myeloma.4 Active in vivo.

[freemexy]

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

CARFILZOMIB

A potent and irreversible proteasome inhibitor. Synthetic analog of the microbial product epoxomcin. 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. Effective against multiple myeloma. Active in vivo.PR171

References:

1. MK Bennett and CJ Kirk Curr. Opin. Drug Disc. Dev. 2008 11:616

2. M Hanada et al. J. Antibiot. (Tokyo) 1992 45:1746

3. SD Demo et al. Cancer Res. 2007 67:6383 4. DJ Kuhn et al. Blood 2007 110:3281

Not for human therapeutic use or for medicinal purposes. For research applications only.