RG7112

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[1].

Product Specifications

CAS Number

[939981-39-2]

Product Name Alternative

RO5045337

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

E1/E2/E3 Enzyme; MDM-2/p53

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/RG7112.html

Purity

99.91

Solubility

DMSO : 200 mg/mL (ultrasonic)

Smiles

C[C@@]1([C@](C)(N(C(C2=CC=C(C=C2OCC)C(C)(C)C)=N1)C(N3CCN(CC3)CCCS(=O)(C)=O)=O)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl

Molecular Formula

C38H48Cl2N4O4S

Molecular Weight

727.78

Precautions

H302, H315, H319, H335

References & Citations

[1]Vu B, et al. Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. ACS Med Chem Lett. 2013 Apr 2;4 (5) :466-9.|[2]Tovar C, et al. MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models. Cancer Res. 2013 Apr 15;73 (8) :2587-97.|[3]Verreault M, et al. Preclinical Efficacy of the MDM2 Inhibitor RG7112 in MDM2-Amplified and TP53 Wild-type Glioblastomas. Clin Cancer Res. 2016 Mar 1;22 (5) :1185-96.