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说明： Potent MDM2 inhibitor; inhibits MDM2-p53 interaction
化学名： 4-[[[(2R,3S,4R,5S)-3-(3-Chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl]carbonyl]amino]-3-methoxybenzoic acid
纯度： ≥98% (HPLC)
生物活性 for Idasanutlin
Idasanutlin is a potent MDM2 inhibitor (IC50 = 6 nM in binding assay, and 30 nM in cancer cell proliferation assay). Induces p53 stabilisation, cell cycle arrest and apoptosis in cancer cells expressing wildtype p53. Displays inhibition of tumor growth in the SJSA1 tumor xenograft model. Also inhibits MDR-1 at high concentrations.
化合物库 for Idasanutlin
Idasanutlin is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Idasanutlin
| 分子量 | 616.49 |
| 公式 | C31H29Cl2F2N3O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1229705-06-9 |
| PubChem ID | 53358942 |
| InChI Key | TVTXCJFHQKSQQM-LJQIRTBHSA-N |
| Smiles | COC1=C(C=CC(C(O)=O)=C1)NC([C@@H]2N[C@H]([C@@]([C@H]2C3=C(C(Cl)=CC=C3)F)(C4=C(C=C(C=C4)Cl)F)C#N)CC(C)(C)C)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Idasanutlin
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 61.65 | 100 |
制备储备液 for Idasanutlin
以下数据基于产品分子量 616.49。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.62 mL | 8.11 mL | 16.22 mL |
| 5 mM | 0.32 mL | 1.62 mL | 3.24 mL |
| 10 mM | 0.16 mL | 0.81 mL | 1.62 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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产品说明书 for Idasanutlin
参考文献 for Idasanutlin
参考文献是支持产品生物活性的出版物。
Ding et al (2013) Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. J.Med.Chem. 56 5979 PMID: 23808545
Chen et al (2014) Structurally diverse MDM2-p53 antagonists act as modulators of MDR-1 function in neuroblastoma. Br.J.Cancer. 111 716 PMID: 24921920
If you know of a relevant reference for Idasanutlin, please let us know.
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关键词: Idasanutlin, Idasanutlin supplier, RG7388, MDM2, inhibitors, mdm2, p53, interaction, Ubiquitin, E3, Ligases, 6904, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
TPD and Induced Proximity Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
Programmed Cell Death Poster
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia