Oprozomib (ONX 0912) - Moligand™, 10mM in DMSO , 26S proteosome inhibitor, CAS No.935888-69-0, 26S proteosome inhibitor

CAS: 935888-69-0 Cat. No.: O408771 Peso molecular: 532.61 PubChem CID: 25067547

GRADE & PURITY Moligand™, 10mM in DMSO

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]-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

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.
In vitro

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 Data

cell lines：

Concentrations：~1 μM

Incubation Time：48 h

Powder Purity:≥99%

Specifications

Sinónimos

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]-

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

26S proteosome inhibitor

Propiedades del producto

• ALogP: 1.1

Nombres e identificadores

• Isómeros SMILES: CC1=NC=C(S1)C(=O)N[C@@H](COC)C(=O)N[C@@H](COC)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)[C@]3(CO3)C
• PubChem CID: 25067547
• Peso molecular: 532.61

Objetivos asociados (humanos)

PSMB5 Tclin Proteasome subunit beta type-5 (4 Activities)

Discover Target: PSMB5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PSMB8 Tclin Proteasome subunit beta type-8 (2 Activities)

Discover Target: PSMB8

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: 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)