卡非佐米

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本试剂(卡非佐米)
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简介：
货 号：LC2-C-3022
名 称：卡非佐米
别 名：Carfilzomib Free Base
C A S ：868540-17-4
分子量：719.91
分子式：C40H57N5O7
纯 度：HPLC/TLC:>99%
说 明：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.
文 献：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).