RO5045337, also known as R7112, RG7112, is a MDM2 antagonist with potential antineoplastic activity. RO5045337 binds to MDM2, thereby preventing the binding of the MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this MDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited and the transcriptional activity of p53 is restored, which may result in the restoration of p53 signaling and thus the p53-mediated induction of tumor cell apoptosis. MDM2, a zinc finger protein, is a negative regulator of the p53 pathway; often overexpressed in cancer cells, it has been implicated in cancer cell proliferation and survival. Check for active clinical trials or closed clinical trials using this agent.
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化学信息
名称 | RO5045337 |
Iupac 化学名称 | ((4S,5R)-2-(4-(tert-butyl)-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethyl-4,5-dihydro-1H-imidazol-1-yl)(4-(3-(methylsulfonyl)propyl)piperazin-1-yl)methanone |
同义词 | R7112 RG7112 |
英文同义词 | R7112 RG7112 |
分子式 | C38H48Cl2N4O4S |
分子量 | 727.78 |
Smile | C(C)(C)(C)C1=CC(=C(C=C1)C=1N([C@]([C@](N1)(C)C1=CC=C(C=C1)Cl)(C)C1=CC=C(C=C1)Cl)C(=O)N1CCN(CC1)CCCS(=O)(=O)C)OCC |
InChiKey | QBGKPEROWUKSBK-QPPIDDCLSA-N |
InChi | InChI=1S/C38H48Cl2N4O4S/c1-8-48-33-26-29(36(2,3)4)14-19-32(33)34-41-37(5,27-10-15-30(39)16-11-27)38(6,28-12-17-31(40)18-13-28)44(34)35(45)43-23-21-42(22-24-43)20-9-25-49(7,46)47/h10-19,26H,8-9,20-25H2,1-7H3/t37-,38+/m0/s1 |
Cas号 | 939981-39-2 |
相关CAS号 | |
外观性状 | Solid powder |
纯度 | 98% by HPLC |
存储 | -20 ºC for 3 years |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature |
海关编码 | |
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Mechanism | |
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