Oprozomib

Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.IC50 value: 36 nM/82 nM(20S proteasome β5/LMP7) [1]Target: 20S proteasomeThe anti-MM activity of Oprozomib is associated with activation of caspase-8, caspase-9, caspase-3, and PARP, as well as inhibition of migration of MM cells and angiogenesis. Oprozomib is demonstrated an absolute bioavailability of up to 39% in rodents and dogs. It is well tolerated wi

Oprozomib has been used in trials studying the treatment of Solid Tumors, Multiple Myeloma, Waldenstrom Macroglobulinemia, Advanced Hepatocellular Carcinoma, and Advanced Non-Central Nervous System (CNS) Malignancies.|Oprozomib is an orally bioavailable proteasome inhibitor with potential antineoplastic activity. Proteasome inhibitor ONX 0912 inhibits the activity of the proteasome, thereby blocking the targeted proteolysis normally performed by the proteasome; this may result in an accumulation of unwanted or misfolded proteins. Disruption of various cell signaling pathways may follow, eventually leading to the induction of apoptosis and inhibition of tumor growth. Proteasomes are large protease complexes that degrade unneeded or damaged proteins that have been ubiquitinated.

Oprozomib is the second class of proteasome inhibitors with higher specificities and reduced toxicities, against head and neck squamous cell carcinoma.

Molecular Weight:532.6
XLogP3:1.1
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:14
Exact Mass:532.19917055
Monoisotopic Mass:532.19917055
Topological Polar Surface Area:177
Heavy Atom Count:37
Complexity:825
Defined Atom Stereocenter Count:4
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes