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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 Basic information |
Product 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 | Synonyms: | [(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;p53 and MDM2 proteins-interaction-inhibitor;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]-;p53 inhibitor;RG7112;RG7112;RG 7112;CS-2164;RO5045337 (RG7112) | CAS: | 939981-39-2 | MF: | C38H48Cl2N4O4S | MW: | 727.78 | EINECS: | | Product Categories: | | Mol File: | 939981-39-2.mol | |
| [(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 Chemical Properties |
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 | color | White to off-white |
| [(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 Usage And Synthesis |
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 |
| [(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 Preparation Products And Raw materials |
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