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说明： Potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1)
化学名： N-[2-(Cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-1H-Imidazole-1-acetamide
纯度： ≥98% (HPLC)
生物活性 for AGI 5198
AGI 5198 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1; IC50 = 70 nM). Selective for mIDH1 over wild-type IDH1 and IDH2. Inhibits production of oncometabolite D-2 hydroxyglutarate. Attenuates growth of glioma cells containing mIDH1, but not wild-type IDH1, in vitro and in vivo. Also inhibits growth of fibrosarcoma and chondrosarcoma cells bearing mIDH1.
化合物库 for AGI 5198
AGI 5198 is also offered as part of the Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for AGI 5198
| 分子量 | 462.56 |
| 公式 | C27H31FN4O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1355326-35-0 |
| PubChem ID | 56645356 |
| InChI Key | FNYGWXSATBUBER-UHFFFAOYSA-N |
| Smiles | CC1=NC=CN1CC(=O)N(C(C(=O)NC1CCCCC1)C1=C(C)C=CC=C1)C1=CC(F)=CC=C1 |
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 AGI 5198
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 23.13 | 50 | |
| ethanol | 4.63 | 10 |
制备储备液 for AGI 5198
以下数据基于产品分子量 462.56。 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 |
|---|---|---|---|
| 0.5 mM | 4.32 mL | 21.62 mL | 43.24 mL |
| 2.5 mM | 0.86 mL | 4.32 mL | 8.65 mL |
| 5 mM | 0.43 mL | 2.16 mL | 4.32 mL |
| 25 mM | 0.09 mL | 0.43 mL | 0.86 mL |
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产品说明书 for AGI 5198
参考文献 for AGI 5198
参考文献是支持产品生物活性的出版物。
Rohle et al (2013) An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells. Science 340 626 PMID: 23558169
Li et al (2015) Treatment with a small molecule mutant IDH1 inhibitor suppresses tumorigenic activity and decreases production of the oncometabolite 2-hydroxyglutarate in human chondrosarcoma cells. PLoS ONE 10 e0133813 PMID: 26368816
Badur et al (2018) Oncogenic R132 IDH1 mutations limit NADPH for de novo lipogenesis through (D)2-hydroxyglutarate production in fibrosarcoma cells. Cell Rep. 25 1018 PMID: 30355481
If you know of a relevant reference for AGI 5198, please let us know.
关键词: AGI 5198, AGI 5198 supplier, AGI5198, potent, selective, inhibitor, inhibits, mutant, isocitrate, dehydrogenase, 1, mIDH1, oncometabolites, D-2, hydroxyglutarate, D-2HG, Isocitrate, (IDH1), 7087, Tocris Bioscience
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该领域的文献
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。
Cancer Metabolism Research Product Guide
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
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- Tricarboxylic Acid Cycle
- Lipidogenesis
- 1C Metabolism and Nucleic Acid Synthesis
- Drivers of Metabolic Reprogramming
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Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Cancer Metabolism Poster
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.