Protein Agonists, Antagonists and Activators

RG-7112 (CAS: 939981-39-2)

Catalog #：EBC52305

Biological Activity

Synonyms

RG7112; RO5045337; RG-7112

Chemical Name

[(4S,5R)-2-(4-tert-butyl-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethylimidazol-1-yl]-[4-(3-methylsulfonylpropyl)piperazin-1-yl]methanone

Application

RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2.

CAS Number

939981-39-2

Purity

≥99.0%

Molecular Weight

727.78

Molecular Formula

C38H48Cl2N4O4S

SMILES

CCOC1=C(C=CC(=C1)C(C)(C)C)C2=NC(C(N2C(=O)N3CCN(CC3)CCCS(=O)(=O)C)(C)C4=CC=C(C=C4)Cl)(C)C5=CC=C(C=C5)Cl

Target & IC50

MDM2: IC50=11 nM

Shipping

Gel Pack

Storage

Store at -20°C

Preparing Stock Solutions

Molecular Structure

ConcentrationSolventMass	1 mg	5 mg	10 mg
1 mM	1.3740 ml	6.8702 ml	13.7404 ml
5 mM	0.2748 ml	1.3740 ml	2.7481 ml
10 mM	0.1374 ml	0.6870 ml	1.3740 ml
50 mM	0.0275 ml	0.1374 ml	0.2748 ml

Solubility
DMSO: 200 mg/mL (274.81 mM)

Product Description

RG7112 is a selective inhibitor of p53-MDM2 binding that frees p53 from negative control, activating the p53 pathway in cancer cells leading to cell cycle arrest and apoptosis. P53 is a potent tumor suppressor that activates the transcription of a subset of genes controlling cell-cycle progression and apoptosis. MDM2 is a negative regulator of p53 that binds the transactivation domain of p53 and inhibits its ability to activate transcription. MDM2 is also an E3 ubiquitin ligase that targets p53 for proteosomal degradation. MDM2 overexpression is one of the mechanisms by which the wild type p53 function is impaired.