Oprozomib
Based on 3 publication(s) in Google Scholar
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.
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- Pureza: 99.76%
- No. CAS: 935888-69-0
- Fòrmula: C25H32N4O7S
- Peso molecular:532.61
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Oprozomib
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | IC50 |
9 nM
Compound: 4
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Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
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[PMID: 30265557] |
| MM1.S | IC50 |
9 nM
Compound: Oprozomib
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Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
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[PMID: 30611983] |
| MV4-11 | IC50 |
28 nM
Compound: 4
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Antiproliferative activity against human MV4-11 cells after 72 hrs by MTS assay
Antiproliferative activity against human MV4-11 cells after 72 hrs by MTS assay
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[PMID: 30265557] |
| MV4-11 | IC50 |
28 nM
Compound: Oprozomib
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Antiproliferative activity against human MV4-11 cells after 72 hrs by MTS assay
Antiproliferative activity against human MV4-11 cells after 72 hrs by MTS assay
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[PMID: 30611983] |
| RPMI-8226 | IC50 |
19 nM
Compound: 4
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Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
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[PMID: 30265557] |
| RPMI-8226 | IC50 |
19 nM
Compound: Oprozomib
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Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
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[PMID: 30611983] |
| RPMI-8226 | IC50 |
31.5 nM
Compound: Oprozomib
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Cytotoxicity activity against human RPMI-8226 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay
Cytotoxicity activity against human RPMI-8226 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay
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[PMID: 33971487] |
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.
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Cell Line:Human MM cell lines (MM.1S, INA-6, RPMI-8226, MM.1R, Dox-40, KMS12, and OPM2)
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Concentration:1, 10, 100, 1000 nM
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Incubation Time:48 hours
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Result:Exhibited anti-MM activity.
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Cell Line:MM.1S cells
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Concentration:7 nM and 10 nM
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Incubation Time:48 hours
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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.
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.
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Animal Model:C57Bl/6 and NOD.SCID.IL2Rγ-/- mice bearing established human RPMI-8226-luc myeloma cells[3]
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Dosage:30 mg/kg
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Administration:Oral gavage once daily for 5 consecutive days followed by 2 days of rest
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Result:Decreased human MM tumor burden and protects mice from bone destruction.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 935888-69-0
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Appearance Solid
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Peso molecular 532.61
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Fòrmula C25H32N4O7S
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Color White to off-white
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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
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Synonyms
ONX 0912; PR-047
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Eur J Pharmacol
Doxorubicin-mediated retardation of aggresome formation enhances Carfilzomib-induced cell death synergistically by augmenting ER stress and proapoptotic signaling. [Abstract]2025 Dec 5:1008:178303. PMID: 41183585 -
Antimicrob Agents Chemother
Inhibitors of the 20S proteasome β5 subunit as potent and selective agents against Trichomonas vaginalis. [Abstract]2025 Dec 10;69(12):e0089325. PMID: 41218108 -
Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Han-Jie Zhou, et al. Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047). J Med Chem. 2009 May 14;52(9):3028-38. [Content Brief]
[2]. Dharminder Chauhan,et al. A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma. Blood. 2010 Dec 2;116(23):4906-15. [Content Brief]
[3]. M A Hurchla, et al.The epoxyketone-based proteasome inhibitors carfilzomib and orally bioavailable oprozomib have anti-resorptive and bone-anabolic activity in addition to anti-myeloma effects. Leukemia. 2013 Feb;27(2):430-40. [Content Brief]
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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