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Oprozomib;ONX-0912

(CAS No:935888-69-0)
Oprozomib (ONX 0912) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.
CAS No:935888-69-0
Molecular Weight(MW):532.61
Purity:98.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 935888-69-0
Molecular formula(MF) C25H32N4O7S
Molecular Weight(MW): 532.61
Alias
Solubility
In vitro DMSO 100 mg/mL (187.75 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
Biological Activity
Description Oprozomib (ONX 0912) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.
Targets
20S proteasome β5 [1] 20S proteasome LMP7 [1]
36 nM 82 nM
In vitro

The 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. [2]

In vivo Oprozomib is demonstrated an absolute bioavailability of up to 39% in rodents and dogs. It is well tolerated with repeated oral administration at doses resulting in >80% proteasome inhibition in most tissues and elicited an antitumor response in multiple human tumor xenograft and mouse syngeneic models [1].