C-3022 Carfilzomib, Free Base, >99%

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 80 mg/mL; soluble in ethanol at 25 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 1-5 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.

CFZ-106 CFZ-105 CFZ-104 CFZ-103 CFZ-102 CFZ-101

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• Carfilzomib, also known as PR-171, is an irreversible, epoxomicin-related proteasome inhibitor. It potently bound to and specifically inhibited the chymotrypsin-like proteasome (ChT-L) and immunoproteasome activities in the β5 subunit with >80% inhibition at doses of ≥10 nM. It showed little or no effect on the postglutamyl peptide hydrolyzing (PGPH) activity in the β1 subunit and trypsin-like (T-L) activity in the β2 subunit at doses of ≤100 nM in vitro. It also inhibited the proliferation of IL-6-independent and -dependent myeloma cell lines with an IC50 of <5 nM in both and ultimately led to apoptosis. Carfilzomib demonstrated higher efficacy compared with bortezomib (please see Cat. No. B-1408, Bortezomib, Free Base) and was active against bortezomib-resistant MM cell lines and samples from patients with clinical bortezomib resistance. Furthermore, carfilzomib overcame resistance to other conventional agents. Kuhn, D.J., et al. "Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma." Blood 110: 3281-3290 (2007).
• Coadministration of carfilzomib with the histone deacetylase inhibitor vorinostat (please see Cat. No. V-8477, Vorinostat) resulted in sharp increases in mitochondrial injury and apoptosis in multiple mantle cell lymphoma (MCL) cell lines and primary MCL cells. Carfilzomib/vorinostat coadministration also induced a pronounced reduction in tumor growth compared with single agent treatment in an MCL xenograft model. Dasmahapatra, G., et al. "Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo." Mol. Cancer Ther. 10: 1686-1697 (2011).
• The response data for single-agent carfilzomib were very promising in bortezomib-naive patients with relapsed and/or refractory multiple myeloma in a phase 2 clinical trial. Vij, R., et al. "An open-label, single-arm, phase 2 (PX-171-004) study of single-agent carfilzomib in bortezomib-naive patients with relapsed and/or refractory multiple myeloma." Blood 119: 5661-5670 (2012).
• Carfilzomib is the active ingredient in the drug product sold under the trade name Kyprolis®. This drug is currently approved in at least one country for use in patients with multiple myeloma. NOTE: THE CARFILZOMIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT KYPROLIS®, AND IS NOT FOR HUMAN USE.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
• Not available in some countries; not available to some institutions; not available for some uses.