1. Metabolic Enzyme/Protease
    Autophagy
  2. Proteasome
    Autophagy

Oprozomib (Synonyms: ONX 0912; PR-047)

Cat. No.: HY-12113 Purity: 99.60%
Handling Instructions

Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.

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
10 mM * 1 mL in DMSO USD 169 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
50 mg USD 576 In-stock
Estimated Time of Arrival: December 31
100 mg USD 720 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. IC50 value: 36 nM/82 nM(20S proteasome β5/LMP7) [1] Target: 20S proteasome 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. 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.

Clinical Trial
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    90% corn oil

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

  • 2.

    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

  • 3.

    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

References
Molecular Weight

532.61

Formula

C₂₅H₃₂N₄O₇S

CAS No.

935888-69-0

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.60%

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Oprozomib
Cat. No.:
HY-12113
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Oprozomib

Cat. No.: HY-12113