Carfilzomib

Name: Carfilzomib
Brand: Tocris Bioscience
SKU: 7188
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 7188

(1)

Citations (5)

COA / SDS

Potent irreversible proteasome inhibitor; active in vivo

Key Product Details

Description:	Potent irreversible proteasome inhibitor; active in vivo
Alternative Names:	PR-171
Chemical Name:	(αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide
Purity:	≥98% (HPLC)
Molecular Weight:	719.92

View Full Technical Details for Carfilzomib

Technical Data
Citations / Reviews (1)

Biological Activity for Carfilzomib

Carfilzomib is a potent irreversible proteasome inhibitor. Preferentially inhibits the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC₅₀ = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC₅₀ = 14 nM) in vitro with minimal cross-reactivity to other proteases. Exhibits little or no effect on PGPH and T-L activities. Activates prosurvival autophagy and induces cell apoptosis. Acts synergistically with dexamethasone (Cat. No. 1126). Suppresses tumor growth in an in vivo xenograft model. Decreases bone resorption and enhances bone formation in non-tumor bearing mice.

Technical Data for Carfilzomib

M. Wt	719.92
Formula	C₄₀H₅₇N₅O₇
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	868540-17-4
PubChem ID	11556711
InChi Key	BLMPQMFVWMYDKT-NZTKNTHTSA-N
Smiles	CC(C)C[C@H](NC(=O)[C@H](CCC1=CC=CC=C1)NC(=O)CN1CCOCC1)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Carfilzomib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	71.99	100
	ethanol	14.4	20

Preparing Stock Solutions for Carfilzomib

The following data is based on the product molecular weight 719.92.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.39 mL	6.95 mL	13.89 mL
5 mM	0.28 mL	1.39 mL	2.78 mL
10 mM	0.14 mL	0.69 mL	1.39 mL
50 mM	0.03 mL	0.14 mL	0.28 mL

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References for Carfilzomib

References are publications that support the biological activity of the product.

Wang Fast identification of possible drug treatment of coronavirus disease-19 (COVID-19) through computational drug repurposing study. J.Chem.Inf.Model 2020 PMID: 32315171
Zhou Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047). J.Med.Chem. 2009 PMID: 19348473
Dou Overview of proteasome inhibitor-based anti-cancer therapies: perspective on bortezomib and second generation proteasome inhibitors versus future generation inhibitors of ubiquitin-proteasome system. Curr.Cancer Drug Targets 2014 PMID: 25092212
Demo Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome. Cancer Res. 2007 PMID: 17616698