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Oprozomib

Chemical Structure : Oprozomib

CAS No.: 935888-69-0

Oprozomib (ONX-0912, ONX0912, PR-047, PR047)

Catalog No.: PC-42896Not For Human Use, Lab Use Only.

Oprozomib (ONX-0912, PR-047) is a potent, orally bioavailable proteasome inhibitor that inhibits chymotrypsin-like (CT-L) activity of 20S proteasome β5/LMP7 with IC50 of 36/82 nM.

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Biological Activity

Oprozomib (ONX-0912, PR-047) is a potent, orally bioavailable proteasome inhibitor that inhibits chymotrypsin-like (CT-L) activity of 20S proteasome β5/LMP7 with IC50 of 36/82 nM.
Oprozomib triggers apoptosis in MM cells, associated with PARP cleavage and caspase activation, causes in vitro and in vivo cytotoxicity in multiple myeloma.
Oprozomib also enhances anti-MM activity of bortezomib, lenalidomide dexamethasone, or pan-histone deacetylase inhibitor.

Physicochemical Properties

M.Wt 532.6092
Formula C25H32N4O7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 50 mg/mL

Chemical Name/SMILES

L-Serinamide, O-methyl-N-[(2-methyl-5-thiazolyl)carbonyl]-L-seryl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-

References

1. Verbrugge SE, et al. J Pharmacol Exp Ther. 2012 Apr;341(1):174-82.

2. Chauhan D, et al. Blood. 2010 Dec 2;116(23):4906-15.

3. Zhou HJ, et al. J Med Chem. 2009 May 14;52(9):3028-38.

4. Hurchla MA, et al. Leukemia. 2013 Feb;27(2):430-40.

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