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Chemical Structure| 935888-69-0 Chemical Structure| 935888-69-0

Structure of Oprozomib
CAS No.: 935888-69-0

Chemical Structure| 935888-69-0

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ONX 0912 is an inhibitor of proteasome that targets the chymotrypsin-like activity of the 20S proteasome subunits β5 (IC50 = 36 nM) and LMP7 (IC50 = 82 nM).

Synonyms: PR-047; ONX 0912

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Product Details of Oprozomib

CAS No. :935888-69-0
Formula : C25H32N4O7S
M.W : 532.61
SMILES Code : C[C@]1(OC1)C([C@H](CC2=CC=CC=C2)NC([C@@H](NC([C@@H](NC(C3=CN=C(C)S3)=O)COC)=O)COC)=O)=O
Synonyms :
PR-047; ONX 0912
MDL No. :MFCD25976563
InChI Key :SWZXEVABPLUDIO-WSZYKNRRSA-N
Pubchem ID :25067547

Safety of Oprozomib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • 20S proteasome

    20S proteasome β5, IC50:36 nM

    20S proteasome LMP7, IC50:82 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
human OCs 25.88 nM 21 days To evaluate the inhibitory effect of Oprozomib on osteoclast differentiation, results showed that Oprozomib significantly inhibited the formation of osteoclasts. PMC3771507
Human 26S proteasome 0.5 mM 30 minutes To investigate the effect of Oprozomib on the structure of the 26S proteasome, it was found that drug binding modifies the energy landscape of conformational motion in the proteasome regulatory particle (RP), resulting in the stabilization of a non-productive state. PMC5458511
MM cell lines 50 nM 4 hours To evaluate the cytotoxic effect of Oprozomib under transient dosing conditions, results showed that Oprozomib effectively inhibited the survival of multiple myeloma cells even after short-term exposure. PMC3771507
human MM cell lines 25 nM 48 hours To evaluate the cytotoxic effect of Oprozomib on human multiple myeloma cells, results showed that Oprozomib exhibited significant cytotoxicity. PMC3771507
acute lymphoblastic leukemia cells 19.2 nM 96 hours To evaluate the cytotoxic effect of ONX 0912 on acute lymphoblastic leukemia cells, the results showed that the LC50 of ONX 0912 for ALL cells was 19.2 nM. PMC3856965
acute myeloid leukemia cells 93.7 nM 96 hours To evaluate the cytotoxic effect of ONX 0912 on acute myeloid leukemia cells, the results showed that the LC50 of ONX 0912 for AML cells was 93.7 nM. PMC3856965
Chronic myeloid leukemia bone marrow mononuclear cells 0.15 to 0.35 μM 48 hours To select the most efficient chemical to induce apoptosis in leukemia cells, a multi-drug screen was applied on bone marrow mononuclear cells from chronic myeloid leukemia (CML) patients. Oprozomib (Cpd 21) was chosen for the subsequent experiments. PMC7780017

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice non-tumor bearing mice Oral gavage 30 mg/kg once daily for 5 consecutive days followed by 2 days of rest for 2 weeks To evaluate the effect of Oprozomib on bone metabolism in non-tumor bearing mice, results showed that Oprozomib significantly increased trabecular bone volume, decreased bone resorption and enhanced bone formation. PMC3771507

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01129349 Solid Tumors PHASE1 COMPLETED 2025-03-13 Oncology Research Associates, ... More >>Scottsdale, Arizona, 85258, United States|Sarah Cannon Research Institute, Nashville, Tennessee, United States|South Texas Accelerated Research Therapeutics, San Antonio, Texas, 78229, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.39mL

1.88mL

0.94mL

18.78mL

3.76mL

1.88mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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