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| SKU | Size | Availability |
Price | Qty |
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O408771-1ml
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1ml |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$391.90
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20S proteasome Selective Inhibitors
| Synonyms | PR-047 | L-Serinamide, O-methyl-N-[(2-methyl-5-thiazolyl)carbonyl]-L-seryl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]- |
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| Specifications & Purity | Moligand™, 10mM in DMSO |
| Biochemical and Physiological Mechanisms | Oprozomib (ONX 0912, PR-047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2. |
| Storage Temp | Store at -80°C |
| Shipped In |
Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available. |
| Grade | Moligand™ |
| Action Type | INHIBITOR |
| Mechanism of action | 26S proteosome inhibitor |
| Product Description |
Information Oprozomib (ONX 0912, PR-047) is an orally bioavailable inhibitor for CT-L activity of20S proteasomeβ5/LMP7 withIC50of 36 nM/82 nM. Phase 1/2. 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. 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 . cell lines: Concentrations:~1 μM Incubation Time:48 h Powder Purity:≥99% |
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Smiles | COCC(NC(=O)C(COC)NC(=O)C1=CN=C(C)S1)C(=O)NC(CC2=CC=CC=C2)C(=O)C3(C)CO3 |
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| Molecular Weight | 532.61 |
| Solubility | Solubility (25°C) In vitro DMSO: 28 mg/mL (200.54 mM); Water: 28 mg/mL (200.54 mM); Ethanol: 28 mg/mL (200.54 mM); |
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