| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R407904-1ml |
1ml |
现货  |
|
| 英文别名 | RO5045337 | ((4S,5R)-2-(4-tert-butyl-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethyl-4,5-dihydroimidazol-1-yl)(4-(3-(methylsulfonyl)propyl)piperazin-1-yl)methanone |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | RG-7112 |
| 生化机理 | RG7112 (RO5045337) 是一种口服生物可用性和选择性 p53-MDM2 抑制剂，其 HTRF IC50 为 18 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | MDM2 原癌基因抑制剂 |
| 产品介绍 |
Information RG-7112 RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM. RG7112 is a potent and selective member of the nutlin family of MDM2 antagonists currently in phase I clinical studies. RG7112 binds MDM2 with high affinity (KD of 10.7 nM), blocking its interactions with p53 in vitro. A crystal structure of the RG7112–MDM2 complex reveals that the small molecule binds in the p53 pocket of MDM2, mimicking the interactions of critical p53 amino acid residues. Treatment of cancer cells expressing wild-type p53 with RG7112 activates the p53 pathway, leading to cell-cycle arrest and apoptosis. RG7112 shows potent antitumor activity against a panel of solid tumor cell lines. However, its apoptotic activity varies widely with the best response observed in osteosarcoma cells with MDM2 gene amplification. In vivo RG7112 activates p53 pathway and induces apoptosis in tumor cells in vivo. Oral administration of RG7112 to human xenograft-bearing mice at nontoxic concentrations caused dose-dependent changes in proliferation/apoptosis biomarkers as well as tumor inhibition and regression. Notably, RG7112 is highly synergistic with androgen deprivation in LNCaP xenograft tumors. cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CCOC1=C(C=CC(=C1)C(C)(C)C)C2=NC(C)(C3=CC=C(Cl)C=C3)C(C)(N2C(=O)N4CCN(CCC[S](C)(=O)=O)CC4)C5=CC=C(Cl)C=C5 |
| 分子量 | 726.28 |
| Concentration | |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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