Carfilzomib is a selective, irreversible proteasome inhibitor (over 80% inhibition at doses of 10 nM and above). In models of multiple myeloma, Carfilzomib potently bound and specifically inhibited the chymotrypsin-like proteasome and immunoproteasome activities, resulting in accumulation of ubiquitinated substrates. It induced a dose- and time-dependent inhibition of proliferation, ultimately leading to apoptosis. It also inhibited proliferation and activated apoptosis in patient-derived MM cells and neoplastic cells from patients with other hematologic malignancies. Carfilzomib showed increased efficacy compared with bortezomib and was active against bortezomib-resistant MM cell lines and samples from patients with clinical bortezomib resistance. Currently it is approved by US FDA for relapsed and refractory multiple myeloma in 2012.
CAS Number: 868540-17-4
Molecular Weight: 719.91
Chemical Name: (S)-4-methyl-N-((S)-1-(((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
Carfilzomib was used at 0.1 µM in vitro and in cellular assays.
Carfilzomib was dosed to mice/rats by intravenous administration at 0.5-4 mg/kg once per day.
- Kuhn DJ, et al. Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. (2007) Blood. 110(9):3281-90.
- Parlati F,et al. Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome. (2009) Blood.114(16):3439-47.
- Dasmahapatra G, et al. Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo. (2011) Mol Cancer Ther. 10(9):1686-97.
- Sacco A, et al. Carfilzomib-dependent selective inhibition of the chymotrypsin-like activity of the proteasome leads to antitumor activity in Waldenstrom's Macroglobulinemia. (2011) Clin Cancer Res. 17(7):1753-64.
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