Carfilzomib (PR-171)

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    An epoxomicin derivate with potential antineoplastic activity. It irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S proteasome, an enzyme responsible for degrading a large variety of cellular proteins. Inhibition of proteasome-mediated proteolysis results in an accumulation of polyubiquinated proteins, which may lead to cell cycle arrest, induction of apoptosis, and inhibition of tumor growth.
    
    1. Guido Cavaletti, et al., Leukemia & Lymphoma (2010), 51 (7), 1178-1187. 2. Girija Dasmahapatra, et al., Blood (2010), 115 (22), 4478-4487.
- Properties
  - Alternative Name
    
    PR 171, PR171, PR-171, Carfilzomib; (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
    
    CAS Number
    
    868540-17-4
    
    Molecular Formula
    
    C40H57N5O7
    
    Molecular Weight
    
    719.91
    
    Appearance
    
    A solid
    
    Purity
    
    98.88%
    
    Solubility
    
    ≥35.99 mg/mL in DMSO; insoluble in H2O; ≥2.64 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only
- Reference
  - 1. Hongo A, Kanaseki T, et al. "Upstream Position of Proline Defines Peptide-HLA Class I Repertoire Formation and CD8(+) T Cell Responses." J Immunol. 2019 May 15; 202 (10): 2849-2855. PMID:30936292
    2. Ayse Tarbin Jannuzzi, Gulce Sari, et al. "Proteasomal Inhibition with Bortezomib Causes Selective Autophagy Upregulation and Perinuclear Clustering of Mitochondria in Human Neuronal Cells?." Proceedings 2018, 2 (25), 1583.
    3. Karademir B, Sari G, et al. "Proteomic approach for understanding milder neurotoxicity of Carfilzomib against Bortezomib." Sci Rep. 2018 Nov 5; 8 (1): 16318. PMID:30397214
    4. Uddin MM, Zou Y, et al. "Proteasome inhibition induces IKK-dependent interleukin-8 expression in triple negative breast cancer cells: Opportunity for combination therapy." PLoS One. 2018 Aug 8; 13 (8): e0201858. PMID:30089134
    5. Zheng Y, Liu Q, t al. "Zika virus elicits inflammation to evade antiviral response by cleaving cGAS via NS1-caspase-1 axis." EMBO J. 2018 Jul 31. pii: e99347. PMID:30065070
    6. Liew PL, Huang RL, et al. "Distinct methylation profile of mucinous ovarian carcinoma reveals susceptibility to proteasome inhibitors." Int J Cancer. 2018 Feb 16. PMID:29451304
    7. Farris TR, Zhu B, et al. "Ehrlichia chaffeensis TRP32 Nucleomodulin Function and Localization Is Regulated by NEDD4L-Mediated Ubiquitination." Front Cell Infect Microbiol. 2018 Jan 11; 7: 534. PMID:29376035
    8. Ma?as A, Chen W, et al. "BaxΔ2 sensitizes colorectal cancer cells to proteasome inhibitor-induced cell death." Biochem Biophys Res Commun. 2018 Jan 29; 496 (1): 18-24. PMID:29291406
    9. Yamashita Y, Anczurowski M, et al."HLA-DP(84Gly) constitutively presents endogenous peptides generated by the class I antigen processing pathway." Nat Commun. 2017 May 10; 8: 15244. PMID:28489076
    10. Federspiel JD, Codreanu SG, et al. "Specificity of protein covalent modification by the electrophilic proteasome inhibitor carfilzomib in human cells." Mol Cell PMID:27503896

Carfilzomib (PR-171)

Background

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