Carfilzomib

Tocris Bioscience | Catalog # 7188

Potent irreversible proteasome inhibitor; active in vivo
Tocris Bioscience

Key Product Details

Description

Potent irreversible proteasome inhibitor; active in vivo

Alternative Names

PR-171
View all Proteasome Inhibitors »

Product Description

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.

Product Specifications for Carfilzomib

Molecular Weight

719.92

Formula

C40H57N5O7

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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Product Documents for Carfilzomib

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for Carfilzomib

For research use only

Related Research Areas

Notch Pathway

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  • Apoptosis induction
    Name: MARINA KOUTSIOUMPA
    Species: Human
    Assay Type: In Vitro
    Verified Customer | Posted 10/13/2022
    Combinatorial treatments of carfilzomib with chemotherapeutics led to synergistic apoptotic phenotype in vitro.

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