1. Metabolic Enzyme/Protease
    Autophagy
  2. Proteasome
    Autophagy
  3. Oprozomib

Oprozomib (Synonyms: ONX 0912; PR-047)

Cat. No.: HY-12113 Purity: 99.71%
Handling Instructions

Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC50s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells.

For research use only. We do not sell to patients.

Oprozomib Chemical Structure

Oprozomib Chemical Structure

CAS No. : 935888-69-0

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 186 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 186 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 158 In-stock
Estimated Time of Arrival: December 31
10 mg USD 211 In-stock
Estimated Time of Arrival: December 31
50 mg USD 634 In-stock
Estimated Time of Arrival: December 31
100 mg USD 792 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC50s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells[1].

In Vitro

Oprozomib inhibits 20S chymotrypsin-like (CT-L) with an IC50 of 55 ± 19 nM. Oprozomib inhibits human leukemia Molt-4 cells CT-L with an IC50 of 66 nM[1].
Oprozomib (ONX 0912; 1-1000 nM; 48 hours) significantly decreases the viability of human multiple myeloma (MM) cell lines[2].
The anti-MM activity of Oprozomib is associated with activation of caspase-8, caspase-9, caspase-3, and PARP[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Human MM cell lines (MM.1S, INA-6, RPMI-8226, MM.1R, Dox-40, KMS12, and OPM2)
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 48 hours
Result: Exhibited anti-MM activity.

Western Blot Analysis[2]

Cell Line: MM.1S cells
Concentration: 7 nM and 10 nM
Incubation Time: 48 hours
Result: Treatment with 3nM triggered a marked increase in proteolytic cleavage of PARP, a signature event during apoptosis. Induced cleavage of caspase-3, an upstream activator of PARP. Induced activation of both casapse-8 (extrinsic) and caspase-9 (intrinsic) apoptotic pathways.
In Vivo

Oprozomib (PR-047) selectively inhibits chymotrypsin-like (CT-L) activity of both the constitutive proteasome (β5) and immunoproteasome (LMP7) and demonstrates an absolute bioavailability of up to 39% in rodents and dogs[1].
Oprozomib promotes antitumor activity in multiple animal models by oral administration at doses below the maximum tolerated dose (MTD)[1].
Oprozomib (30 mg/kg by oral gavage once daily for 5 consecutive days followed by 2 days of rest) treatment decreases tumor burden in C57Bl/6 and NOD.SCID.IL2Rγ-/- mice[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57Bl/6 and NOD.SCID.IL2Rγ-/- mice bearing established human RPMI-8226-luc myeloma cells[3]
Dosage: 30 mg/kg
Administration: Oral gavage once daily for 5 consecutive days followed by 2 days of rest
Result: Decreased human MM tumor burden and protects mice from bone destruction.
Clinical Trial
Molecular Weight

532.61

Formula

C25H32N4O7S

CAS No.
SMILES

C[[email protected]]1(OC1)C([[email protected]](CC2=CC=CC=C2)NC([[email protected]@H](NC([[email protected]@H](NC(C3=CN=C(C)S3)=O)COC)=O)COC)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (93.88 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8775 mL 9.3877 mL 18.7755 mL
5 mM 0.3755 mL 1.8775 mL 3.7551 mL
10 mM 0.1878 mL 0.9388 mL 1.8775 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 99.71%

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