AdipoGen Life Sciences

Carfilzomib [PR-171]

CHF 40.00

In stock

AG-CR1-3669-M0011 mgCHF 40.00

AG-CR1-3669-M0055 mgCHF 65.00

AG-CR1-3669-M02525 mgCHF 110.00

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Product Details
Synonyms	(αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide
Product Type	Chemical
Properties
Formula	C₄₀H₅₇N₅O₇
MW	719.9
CAS	868540-17-4
Purity Chemicals	≥98% (HPLC)
Appearance	White solid.
Solubility	Soluble in DMSO (30mg/ml) or EtOH (20mg/ml). Poorly soluble in aqueous buffers.
Other Product Data	Note: Warming and sonication may be required when dissolving the compound in the solvent of choice. Stock solutions are stable for at least 1 month when stored at -20°C.
InChi Key	BLMPQMFVWMYDKT-NZTKNTHTSA-N
Smiles	O=C([C@]1(C)OC1)[C@H](CC(C)C)NC([C@H](CC2=CC=CC=C2)NC([C@H](CC(C)C)NC([C@H](CCC3=CC=CC=C3)NC(CN4CCOCC4)=O)=O)=O)=O
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Handling Advice	Keep cool and dry.
Use/Stability	Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS	Download PDF
Product Specification Sheet
Datasheet	Download PDF

Product-specific References

Description

Potent and irreversible second-generation peptide epoxyketone class proteasome inhibitor. Synthetic analog of the microbial product epoxomicin (Prod. No. AG-CN2-0422).
Targets the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC₅₀=5.2nM) and the β5i subunit [LMP7] of the 20S immunoproteasome (IC₅₀=14nM), with minimal cross-reactivity to other proteases.
Displays equal potency but greater selectivity for the chymotrypsin-like activity of the proteasome compared to bortezomib (Prod. No. AG-CR1-3602).
Anticancer compound effective against multiple myeloma in vivo.
In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, lymphoma and various solid tumors (IC₅₀s=2.4-20nM).

Product References

Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome: S.D. Demo, et al.; Cancer Res. 67, 6383 (2007)
Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma: D.J. Kuhn, et al.; Blood 110, 3281 (2007)
The proteasome inhibitors bortezomib and PR-171 have antiproliferative and proapoptotic effects on primary human acute myeloid leukaemia cells: C. Stapnes, et al.; Br. J. Haematol. 136, 814 (2007)
Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome: F. Parlati, et al.; Blood 114, 3439 (2009)
Second generation proteasome inhibitors: carfilzomib and immunoproteasome-specific inhibitors (IPSIs): D.J. Kuhn, et al.; Curr. Cancer Drug Targets 11, 285 (2011) (Review)
Carfilzomib-dependent selective inhibition of the chymotrypsin-like activity of the proteasome leads to antitumor activity in Waldenstrom's Macroglobulinemia: A. Sacco, et al.; Clin. Cancer Res. 17, 1753 (2011)
Nonproteasomal targets of the proteasome inhibitors bortezomib and carfilzomib: a link to clinical adverse events: S. Arastu-Kapur, et al.; Clin. Cancer Res. 17, 2734 (2011)
Carfilzomib: a novel second-generation proteasome inhibitor: M.L. Khan & A.K. Stewart; Future Oncol. 7, 607 (2011)
The next generation proteasome inhibitors carfilzomib and oprozomib activate prosurvival autophagy via induction of the unfolded protein response and ATF4: Y. Zang, et al.; Autophagy 8, 1873 (2012)
From epoxomicin to carfilzomib: chemistry, biology, and medical outcomes: K.B. Kim & C.M. Crews; Nat. Prod. Rep. 30, 600 (2013)
In vitro and in vivo therapeutic efficacy of carfilzomib in mantle cell lymphoma: targeting the immunoproteasome: L. Zhang, et al.; Mol. Cancer Ther. 12, 2494 (2013)
Carfilzomib for the treatment of patients with relapsed and/or refractory multiple myeloma: A.K. Stewart; Future Oncol. 11, 2121 (2015)
Carfilzomib Inhibits Constitutive NF-κB Activation in Mantle Cell Lymphoma B Cells and Leads to the Induction of Apoptosis: Y.L. Zhang, et al.; Acta Haematol. 137, 106 (2017)

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