RG7112D

RG7112D is a potent MDM2 inhibitor with IC50s of 11 nM and >10000 nM and for MDM2-p53 and VHL-HIF1α by binding HTRF assay, respectively. RG7112D is coupled by an amide bond to VHL-Amine, resulting in a bi-functional molecule, YX-02-030. YX-02-03, a MDM2-PROTAC, potently inhibits MDM2-p53 binding (HTRF IC50=63nM) . RG7112D can stabilize MDM2 protein and increase p53 protein levels[1].

Product Specifications

CAS Number

[2360561-90-4]

UNSPSC

12352005

Target

MDM-2/p53

Type

Reference compound

Related Pathways

Apoptosis

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/rg7112d.html

Smiles

O=C(CN1CCN(CC1)C(N2[C@](C3=CC=C(C=C3)Cl)([C@](C4=CC=C(C=C4)Cl)(N=C2C5=CC=C(C=C5OCC)C(C)(C)C)C)C)=O)O

Molecular Formula

C36H42Cl2N4O4

Molecular Weight

665.65

References & Citations

[1]Clare M Adams, et al. Targeted MDM2 Degradation Reveals a New Vulnerability for p53-Inactivated Triple-Negative Breast Cancer. Cancer Discov. 2023 May 4;13 (5) :1210-1229.