Carfilzomib Inhibitor CAS No. 868540-17-4

Cat. No.	Name	Size	Price
KI3119	Carfilzomib	5 mg	$272
	Carfilzomib	10 mg	$432
	Carfilzomib	50 mg	$1072
	Carfilzomib	100 mg	$1392

Chemical Characteristic

Product Name	Carfilzomib
CAS No.	868540-17-4
Molecular Weight	719.9099
Formula	C₄₀H₅₇N₅O₇
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
Smiles	C(=O)(C(NC(=O)C(NC(=O)[C@H](CCc1ccccc1)NC(=O)CN1CCOCC1)CC(C)C)Cc1ccccc1)NC(C(=O)[C@@]1(OC1)C)CC(C)C
Chemical Structure

Biological activities

Carfilzomib is a novel, irreversible and epoxomicin-related proteasome inhibitor. Carfilzomib inhibits the chymotrypsin activity of purified constitutive 20S proteasome and the chymotrypsin activity of the immunoproteasome with IC50s of 6 and 33 nM, respectively.^[1] Carfilzomib treatment for 24 hours, dose-dependently decreases viability of ANBL-6, RPMI 8226, U266 and KAS-6/1 cells, with IC50s less than 5 nM. Carfilzomib overcomes dexamethasone (Dex)-resistance (MM1.R) cells and parental MM1.S cells with IC50s of 15.2 and 29.3 nM, respectively. Carfilzomib inhibits the chymotrypsin-like activity of the proteasome both in vitro and in cellulo in models of multiple myeloma (MM). Carfilzomib inhibits proliferation in a variety of cell lines and human neoplastic cells, including MM. Carfilzomib induces intrinsic and extrinsic apoptotic signaling pathways and activation of c-Jun-N-terminal kinase (JNK). Carfilzomib acts synergistically with dexamethasone to enhance cell death.^[2] Carfilzomib selectively inhibits both chymotrypsin-like active sites b5 and low molecular mass protein-7 (LMP-7), and induces an antitumor response in MM, non-Hodgkin lymphoma (NHL), and leukemia cells with minimal cytotoxic effects in nontransformed cells.^[3] Importantly, carfilzomib targets Waldenstrom?? Macroglobulinemia (WM) cells even in the context of bone marrow (BM) milieu. In vivo, carfilzomib can lower IgM secretion in the serum of mice.^[1]

Protocols

In vitro, carfilzomib is dissolved in DMSO.^[2]

References

[1] Sacco A, et al. Carfilzomib-dependent selective inhibition of the chymotrypsin- like activity of the proteasome leads to antitumor activity in Waldenstrom's Macroglobulinemia. Clin Cancer Res. 2011, 17(7): 1753-1764. [2] Kuhn DJ, et al. Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. Blood. 2007, 110(9): 3281-3290. [3] Parlati F, et al. Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome. Blood. 2009, 114(16): 3439-3447.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com