RG-7112 - Moligand™, 10mM in DMSO , Inhibitor of MDM2 proto-oncogene, CAS No.939981-39-2, Inhibitor of MDM2 proto-oncogene

CAS: 939981-39-2 Cat. No.: R407904 Peso molecular: 727.78 PubChem CID: 57406853

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

RO5045337 | ((4S,5R)-2-(4-tert-butyl-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazol-1-yl)(4-(3-(methylsulfonyl)propyl)piperazin-1-yl)methanone

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

RG-7112 RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.
In vitro

RG7112 is a potent and selective member of the nutlin family of MDM2 antagonists currently in phase I clinical studies. RG7112 binds MDM2 with high affinity (K_D of 10.7 nM), blocking its interactions with p53 in vitro. A crystal structure of the RG7112–MDM2 complex reveals that the small molecule binds in the p53 pocket of MDM2, mimicking the interactions of critical p53 amino acid residues. Treatment of cancer cells expressing wild-type p53 with RG7112 activates the p53 pathway, leading to cell-cycle arrest and apoptosis. RG7112 shows potent antitumor activity against a panel of solid tumor cell lines. However, its apoptotic activity varies widely with the best response observed in osteosarcoma cells with MDM2 gene amplification.

In vivo

RG7112 activates p53 pathway and induces apoptosis in tumor cells in vivo. Oral administration of RG7112 to human xenograft-bearing mice at nontoxic concentrations caused dose-dependent changes in proliferation/apoptosis biomarkers as well as tumor inhibition and regression. Notably, RG7112 is highly synergistic with androgen deprivation in LNCaP xenograft tumors.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

RO5045337 | ((4S, 5R)-2-(4-tert-butyl-2-ethoxyphenyl)-4, 5-bis(4-chlorophenyl)-4, 5-dimethyl-4, 5-dihydroimidazol-1-yl)(4-(3-(methylsulfonyl)propyl)piperazin-1-yl)methanone

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.

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

Inhibitor of MDM2 proto-oncogene

Nombres e identificadores

• Isómeros SMILES: CCOC1=C(C=CC(=C1)C(C)(C)C)C2=N[C@@]([C@@](N2C(=O)N3CCN(CC3)CCCS(=O)(=O)C)(C)C4=CC=C(C=C4)Cl)(C)C5=CC=C(C=C5)Cl
• CAS alternativo: 939981-39-2
• PubChem CID: 57406853
• Términos de entrada MeSH: RG7112
• Peso molecular: 727.78

Objetivos asociados (humanos)

MDM2 Tchem E3 ubiquitin-protein ligase Mdm2 (4 Activities)

Discover Target: MDM2

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