ChemicalBook--->CAS DataBase List--->939981-39-2

939981-39-2

939981-39-2 Structure

939981-39-2 Structure
IdentificationBack Directory
[Name]

[(4R,5S)-4,5-Bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone
[CAS]

939981-39-2
[Synonyms]

RG7112
CS-2164
p53 inhibitor
RG7112;RG 7112
RG7112(RO5045337)
RO5045337 (RG7112)
p53 and MDM2 proteins-interaction-inhibitor
[(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
[(4R,5S)-4,5-Bis(4-chlorophenyl)-2-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-dimethyl-1H-imidazol-1-yl][4-[3-(methylsulfonyl)propyl]-1-piperazinyl]methanone
Methanone, [(4S,5R)-4,5-bis(4-chlorophenyl)-2-[4-(1,1-diMethylethyl)-2-ethoxyphenyl]-4,5-dihydro-4,5-diMethyl-1H-iMidazol-1-yl][4-[3-(Methylsulfonyl)propyl]-1-piperazinyl]-
[Molecular Formula]

C38H48Cl2N4O4S
[MDL Number]

MFCD29905459
[MOL File]

939981-39-2.mol
[Molecular Weight]

727.78
Chemical PropertiesBack Directory
[density ]

1.23
[storage temp. ]

Store at -20°C
[solubility ]

≥36.4 mg/mL in DMSO; insoluble in H2O; ≥31.87 mg/mL in EtOH
[form ]

solid
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
Hazard InformationBack Directory
[Description]

RG-7112 is an inhibitor of mouse double-minute 2 protein (MDM2; IC50 = 0.018 μM), an E3 ubiquitin ligase that ubiquitinates the tumor suppressor p53 and also acts as a negative regulator of p53 transcriptional activity. RG-7112 binds to the p53 binding pocket of MDM2. It increases the levels of p53 and its transcriptional targets in SJSA-1 osteosarcoma cells. It inhibits proliferation in cancer cell lines expressing wild-type p53 (IC50s = 0.18-2.2 μM) and cell lines expressing mutant p53 (IC50s = 5.7-20.3 μM). RG-7112 also prevents and reduces tumor growth in an SJSA-1 mouse xenograft model when administered at doses of 50 and 100 mg/kg per day, respectively. However, it inhibits thrombopoiesis in vivo, decreasing platelet counts in rats when administered at doses of 50 and 100 mg/kg and in cynomolgus monkeys at doses of 10 and 20 mg/kg.
[Uses]

RG 7112 is MDM2 antagonist. It can be used in biological study of single mouse analysis on evaluation of alternative in vivo drug screening methodology.
[target]

MDM2
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