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 分子式: C₃₈H₄₈Cl₂N₄O₄S 分子量: 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

概要

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

同義語

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

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

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

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

INHIBITOR

作用メカニズム

Inhibitor of MDM2 proto-oncogene

名前と識別子

• 異性体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
• 代替CAS番号: 939981-39-2
• PubChem CID: 57406853
• MeSH用語: RG7112
• 分子量: 727.78

関連ターゲット（人間）

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)

よくある質問

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 939981-39-2, the molecular formula is C38H48Cl2N4O4S, and the molecular weight is 727.78 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.