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- CAS号：
939981-39-2
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ￥334.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥1168.0 |
| 规格： | 5mg | 产品价格： | ￥713.0 |
| 规格： | 10mg | 产品价格： | ￥1056.0 |
| 规格： | 25mg | 产品价格： | ￥2096.0 |
| 规格： | 50mg | 产品价格： | ￥3104.0 |
| 规格： | 100mg | 产品价格： | ￥4424.0 |
Product Introduction
Bioactivity
| 名称 | RG7112 |
| 描述 | RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor. |
| 细胞实验 | Cell lines: Three wild-type p53 (HCT116,RKO,and SJSA1) and 2 mutant p53 (SW480 and MDA-MB-435) cell lines. Concentrations: ~5 μM. Incubation Time: 5 d. Method: Cell proliferation/viability is evaluated by the tetrazolium dye (MTT) assay.Cell growth kinetics are measured using the IncuCyte live cell imaging system.For cell-cycle analysis,cells are cultured in T75 flask with appropriate growth medium (106 cells/condition in 10 mL) and incubated overnight at 37°C.They are incubated with test compounds and processed. |
| 激酶实验 | HTRF assay: Homogeneous time-resolved fluorescence (HTRF) assay measures the signal generated by 2 components when they are in close proximity. The p53–MDM2 binding assay uses a biotinylated peptide derived from the MDM2-binding domain of p53 and a truncated N-terminal portion of recombinant human GST-tagged MDM2 protein containing the p53-binding domain. Proteins for crystal structure studies are expressed in E. coli strain BL21 using the helper plasmid pUBS 520 coding for the lacIq repressor and the rare tRNAArg [AGA/AGG]. For crystallization, the frozen protein is thawed and concentrated to 9.8 mg/mL using a Centricon concentrator (3,000 MW cutoff). The complex is then formed by combining the protein with a slight molar excess of the inhibitor (stock solution is 100 mM in DMSO) and this solution is allowed to sit for 4 hours at 4°C. Cryopreserved crystals are used to collect diffraction data on beamline X8C at the National Synchrotron Light Source at Brookhaven National Laboratory. |
| 动物实验 | Animal Models: Nude mice bearing SJSA-1,MHMn,or LNCaP xenografts. Formulation: Suspended in 1% Klucel LF/0.1% Tween 80. Dosages: ~200 mg/kg. Administration: p.o. |
| 体外活性 | In three wild-type p53 (HCT116, RKO, and SJSA1) cell lines, RG7112 selectively and dose-dependently inhibits cell growth. In cancer cells expressing wild-type p53, RG7112 activates the p53 pathway, and induces cell-cycle arrest and apoptosis. RG7112, both alone and combined with Peg-IFNα 2a, significantly decreases MPN colony-forming unit-granulocyte macrophage and burst-forming unit-erythroid numbers and preferentially eliminates the total number of JAKV617F(+) MPN hematopoietic progenitor cells. In addition, in MDM2-amplified liposarcoma cells, RG7112 significantly synergizes with Trabectedin. |
| 体内活性 | In rats, RG7112 impairs thrombopoiesis via activation of p53. In the SJSA1 xenograft mouse model, RG7112 (200 mg/kg, p.o.) penetrates tumor cells and activate p53 and its 2 major functions, cell-cycle arrest and apoptosis. In nude mice bearing SJSA-1, and MHMn xenografts, RG7112 (100 mg/kg, p.o.) causes tumor regression. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 93 mg/mL (127.79 mM), Sonication is recommended. 10% DMSO+90% Saline : 10 mg/mL (13.74 mM), Solution. DMSO : 250 mg/mL (343.51 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (13.74 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | Ubiquitin ligase | Ubiquitin conjugating enzyme | Ubiquitin activating enzyme | RO-5045337 | RO 5045337 | RG7112 | MDM-2/p53 | Mdm2 | Inhibitor | inhibit | E3Enzyme | E3 ligating enzyme | E3 Enzyme | E2Enzyme | E2 Enzyme | E2 conjugating enzyme | E1Enzyme | E1/E2/E3 Enzyme | E1 Enzyme | E1 activating enzyme |
| 相关产品 | Methyl methanesulfonate | Diuron | Yucasin | Flubendazole | Thiabendazole | D-(-)-3-Phosphoglyceric acid disodium | 10-Hydroxydecanoic Acid | (E/Z)-10-Hydroxy-2-decenoic acid | Indole-3-carbinol | EN219 | Triglycidyl isocyanurate | Gallium maltolate |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Cancer Metabolism Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Aging Compound Library | Orally Active Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 RG7112【939981-39-2】
￥334 - 4424
