Oprozomib (ONX-0912)

Short Summary : Proteasome inhibitor

Category : Ubiquitination/ Proteasome|Proteasome

Purity : 0.9949

CAS Number : 935888-69-0

Formula : C25H32N4O7S

Molecular Weight : 532.61

SMILE : CC1=NC=C(S1)C(=O)NC(COC)C(=O)NC(COC)C(=O)NC(CC2=CC=CC=C2)C(=O)C3(CO3)C

Solubility : >26.6mg/mL in DMSO

Storage : Desiccate at -20°C

Description : ONX-0912 (as known as oprozomib), discovered during a medicinal chemistry effort using tripeptide epoxyketones, is an orally bio-available and potent proteasome inhibitor that inhibits growth and induces apoptosis in bortezomib resistant multiple myeloma (MM) cells. Although ONX-0912, an analog of carfilzomib, is structurally distinct from bortezomib, it possesses the same ability as bortezomib to predominantly inhibit chymotrypsin-like activity of the proteasome. ONX-0912 exhibits significant anti-MM activities to reduce tumor progression and prolong survival in many animal tumor model studies, which are associated with activation of caspase-3, caspase-8, caspase-9, and poly(ADP) ribose polymerase and inhibition of anglogensis and MM cells migration.
Reference
Dharminder Chauhan, Ajita V. Singh, Monette Aujay, Christopher J. Kirk, Madhavi Bandi, Bryan Ciccarelli, Noopur Raje, Paul Richardson, and Kenneth C. Anderson. A novel oraaly active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma. Blood 2010; 116(23): 4906-4915

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