[(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

Name	RG7112
Synonyms	RG7112 RG 7112 CS-2164 p53 inhibitor RO5045337 (RG7112) p53 and MDM2 proteins-interaction-inhibitor [(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]-
CAS	939981-39-2

Molecular Formula	C38H48Cl2N4O4S
Molar Mass	727.78
Density	1.23
Storage Condition	-20℃
In vitro study	RG7112 is a potent and selective MDM2 antagonist, a member of the Nutlin family, and is currently in Phase I clinical studies. RG7112 binds MDM2 with high affinity (K D of 10.7 nM), blocking its interaction with p53 in vitro. The crystal structure of the RG7112-MDM2 complex indicates that the small molecule binds to the p53 pocket of MDM2, mimicking the interaction of important p53 amino acid residues. Treatment of cancer cells expressing wild-type p53 by RG7112 activates the p53 pathway, leading to cell cycle arrest and apoptosis. RG7112 exhibited potent anti-tumor activity against a panel of tumor cell lines. However, their anti-apoptotic activity was quite different, with optimal responses observed in MDM2 gene-amplified osteosarcoma cells.
In vivo study	RG7112 activates the p53 pathway in vivo and induces tumor cell apoptosis. Oral administration of RG7112 to human xenograft-bearing mice at nontoxic concentrations caused dose-dependent changes in proliferation/apoptosis biomarkers, as well as tumor suppression and regression. Notably, RG7112 was highly synergistic with chemical castration in LNCaP xenograft tumors.

Last Update：2024-01-02 23:10:35

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CAS: 939981-39-2
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Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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[(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 Request for Quotation