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Carfilzomib is an analog of epoxomicin that functions as a proteasome inhibitor. This drug has been approved for use in humans with multiple myeloma. Carfilzomib binds irreversibly to the 20S proteasome, which exhibits chymotrypsin-like activity and is responsible for degradation of cellular proteins; as a result, concentrations of polyubiquitinated proteins build up, inducing cell cycle arrest at the G2/M phase, apoptosis, and decreased tumor growth.
| Cas No. | 868540-17-4 |
|---|---|
| Purity | ≥98% |
| Formula | C40H57N5O7 |
| Formula Wt. | 719.91 |
| Chemical Name | (2S)-4-methyl-N-[(2S)-1-[[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1- oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[(2- morpholin-4-ylacetyl)amino]-4-phenylbutanoyl]amino]pentanamide |
| IUPAC Name | (2S)-4-methyl-N-[(2S)-1-[[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1- oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[(2- morpholin-4-ylacetyl)amino]-4-phenylbutanoyl]amino]pentanamide |
| Synonym | PR-171 |
| Solubility | The solubility of carfilzomib in ethanol is approximately 1 mg/ml and approximately 15 mg/ml in DMSO and DMF. Carfilzomib is sparingly soluble in aqueous solutions. |
| Appearance | white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Gu JJ, Hernandez-Ilizaliturri FJ, Kaufman GP, et al. The novel proteasome inhibitor carfilzomib induces cell cycle arrest, apoptosis and potentiates the anti-tumour activity of chemotherapy in rituximab-resistant lymphoma. Br J Haematol. 2013 Jul 4. Epub ahead of print] PMID: 23826755.
Lee HC, Shah JJ, Orlowski RZ. Novel approaches to treatment of double-refractory multiple myeloma. Am Soc Clin Oncol Educ Book. 2013;2013:302-6. doi: E10.1200/EdBook_AM.2013.33.e302. PMID: 23714530.
Nooka A, Gleason C, Casbourne D, et al. Relapsed and refractory lymphoid neoplasms and multiple myeloma with a focus on carfilzomib. Biologics. 2013;7:13-32. PMID: 23386784