Carfilzomib

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Cat.No. 7188 - Carfilzomib | C40H57N5O7 | CAS No. 868540-17-4
Description: Potent irreversible proteasome inhibitor; active in vivo
Alternative Names: PR-171
Chemical Name:S)-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)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

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

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 Data

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

Preparing Stock Solutions

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.

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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References

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

Demo et al (2007) Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome. Cancer Res. 67 6383 PMID: 17616698

Zhou et al (2009) Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047). J.Med.Chem. 52 3028 PMID: 19348473

Dou et al (2014) 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 14 517 PMID: 25092212

Wang et al (2020) Fast identification of possible drug treatment of coronavirus disease-19 (COVID-19) through computational drug repurposing study. J.Chem.Inf.Model 60 3277 PMID: 32315171


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