Oprozomib (ONX 0912)

Catalog No.S7049

Oprozomib (ONX 0912) Chemical Structure

Molecular Weight(MW): 532.61

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.

Size Price Stock Quantity  
In DMSO USD 310 In stock
USD 147 In stock
USD 970 In stock
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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].

Protocol

Kinase Assay:[3]
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ELISA-based active site binding assay:

Samples (lysed cells or tissue homogenates) are treated for 1 h at room temperature with the biotinylated active site probe PR-584 (5-15 μM). Samples are denatured by addition of SDS (0.9% final) and heating to 100 °C for 5 min. The denatured samples are transferred to a 96-well or 384-well filter plat, mixed with streptavidin-sepharose beads (2.5-5 μL packed beads/well), and incubated for 1 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer (PBS, 1% bovine serum albumin, 0.1% Tween-20) by vacuum filtration. The beads are incubated overnight at 4 °C on a plate shaker with the following antibodies recognizing the six catalytic subunits diluted into ELISA buffer: β5, β1, and β2 diluted 1:3000, LMP7 and LMP2 diluted 1:5000, and MECL-1 diluted 1:1000. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and incubated with HRP-conjugated secondary antibody diluted 1:5000 in ELISA buffer and incubated 2 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and developed for chemiluminsecence signal using the supersignal ELISA pico substrate following the manufacturer's instructions. Luminescence is measured on a plate reader and converted to ng of proteasome or μg/ml of lysate by comparison with 20S proteasome or untreated cell lysate standard curves. For proteasome inhibitor studies, active site probe binding values are expressed as the percent of binding relative to DMSO treated cells.
Cell Research:[2]
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  • Cell lines: MM.1S, MM.1R, RPMI-8226, KMS12, INA-6, OPM-2, Dox-40
  • Concentrations: ~1 μM
  • Incubation Time: 48 h
  • Method: MTT assay
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Non-Hodgkin’s lymphoma cell line RL xenograft, colorectal tumor cell line CT-26 xenograft
  • Formulation: 10% (v/v) EtOH and 10% (v/v) PS80 in citrate buffer (pH 3.5)
  • Dosages: 30 mg/kg, twice weekly on days 1 and 2
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (187.75 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 532.61
Formula

C25H32N4O7S

CAS No. 935888-69-0
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02939183 Recruiting Relapsed or Refractory Multiple Myeloma Amgen January 2017 Phase 1
NCT02227914 Withdrawn Advanced Hepatocellular Carcinoma Onyx Therapeutics, Inc.|Onyx Pharmaceuticals December 2014 Phase 1|Phase 2
NCT02244112 Active, not recruiting Advanced Non-Central Nervous System (CNS) Malignancies Onyx Therapeutics, Inc.|Onyx Pharmaceuticals August 2014 Phase 1
NCT02072863 Completed Multiple Myeloma Onyx Therapeutics, Inc.|Onyx Pharmaceuticals January 2014 Phase 1|Phase 2
NCT01999335 Active, not recruiting Multiple Myeloma Onyx Therapeutics, Inc.|Onyx Pharmaceuticals November 2013 Phase 1|Phase 2
NCT01881789 Active, not recruiting Multiple Myeloma Onyx Therapeutics, Inc.|Onyx Pharmaceuticals August 2013 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID