COA | MSDS | HPLC | NMR |
CAS No: | 935888-69-0 |
Molecular formula(MF) | C25H32N4O7S |
Molecular Weight(MW): | 532.61 |
Alias |
In vitro | DMSO | 100 mg/mL (187.75 mM) |
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Water | <1 mg/mL | |
Ethanol | <1 mg/mL |
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. | ||||
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Targets |
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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] |
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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]. |