| Identification | Back Directory | [Name]
1-Piperazineacetic acid, 4-[[(4S,5R)-4,5-bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl]carbonyl]- | [CAS]
2360561-90-4 | [Synonyms]
RG7112D
1-Piperazineacetic acid, 4-[[(4S,5R)-4,5-bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl]carbonyl]- | [Molecular Formula]
C36H42Cl2N4O4 | [MOL File]
2360561-90-4.mol | [Molecular Weight]
665.65 |
| Hazard Information | Back Directory | [Uses]
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]. | [References]
[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. DOI:10.1158/2159-8290.CD-22-1131 |
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