Carfilzomib

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.

Solubility

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:

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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

Calculators

Background References

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