2. Metabolic Enzyme/Protease Autophagy Apoptosis
  3. Proteasome Autophagy Apoptosis
  4. Oprozomib

Oprozomib  (Synonyms: ONX 0912; PR-047)

Cat. No.: HY-12113 Purity: 99.71%
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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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 185 In-stock
Solution
10 mM * 1 mL in DMSO USD 185 In-stock
Solid
1 mg USD 75 In-stock
5 mg USD 158 In-stock
10 mg USD 211 In-stock
50 mg USD 634 In-stock
100 mg USD 792 In-stock
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Based on 1 publication(s) in Google Scholar

Oprozomib Related Antibodies

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  • Purity & Documentation

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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].

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

Oprozomib Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (93.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.71%

COA (253 KB) LCMS (119 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8775 mL 9.3877 mL 18.7755 mL 46.9387 mL
5 mM 0.3755 mL 1.8775 mL 3.7551 mL 9.3877 mL
10 mM 0.1878 mL 0.9388 mL 1.8775 mL 4.6939 mL
15 mM 0.1252 mL 0.6258 mL 1.2517 mL 3.1292 mL
20 mM 0.0939 mL 0.4694 mL 0.9388 mL 2.3469 mL
25 mM 0.0751 mL 0.3755 mL 0.7510 mL 1.8775 mL
30 mM 0.0626 mL 0.3129 mL 0.6258 mL 1.5646 mL
40 mM 0.0469 mL 0.2347 mL 0.4694 mL 1.1735 mL
50 mM 0.0376 mL 0.1878 mL 0.3755 mL 0.9388 mL
60 mM 0.0313 mL 0.1565 mL 0.3129 mL 0.7823 mL
80 mM 0.0235 mL 0.1173 mL 0.2347 mL 0.5867 mL
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Oprozomib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Oprozomib935888-69-0ONX 0912 PR-047ONX0912ONX-0912PR047PR 047PR-047ProteasomeAutophagyApoptosisorallybioavailableepoxyketoneproteasomeβ5immunoproteasome LMP7apoptosisMMInhibitorinhibitorinhibit

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