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Submit ReviewIvosidenib
说明： Potent inhibitor of mutant isocitrate dehydrogenase (mIDH1)
化学名： (2S)-N-{(1S)-1-(2-Chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl}-1(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
纯度： ≥98% (HPLC)
生物活性 for Ivosidenib
Ivosidenib is a potent inhibitor of mutant isocitrate dehydrogenase enzyme 1 (mIDH1), with activity against a variety of mutant IDH1 enzymes (IC50 range = 5-19 nM). Reduces intracellular 2-HG (Cat. No. 6122) by 96% at 0.5 μM. Increases sensitivity of melanoma to Temozolomide (Cat. No. 2706) in vivo and inhibits wild-type IDH1 in low magnesium and low nutrient levels. Ivosidenib also inhibits growth of tumors in cell and animal models of pancreatic cancer and inhibits invasion and migration of chondrosarcoma cells in vitro.
技术数据 for Ivosidenib
| 分子量 | 582.96 |
| 公式 | C28H22ClF3N6O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1448347-49-6 |
| PubChem ID | 71657455 |
| InChI Key | WIJZXSAJMHAVGX-DHLKQENFSA-N |
| Smiles | N([C@H](C(NC1CC(F)(F)C1)=O)C2=C(Cl)C=CC=C2)(C(=O)[C@H]3N(C(=O)CC3)C4=CC(C#N)=CC=N4)C=5C=C(F)C=NC5 |
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 Ivosidenib
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 58.3 | 100 | |
| ethanol | 58.3 | 100 |
制备储备液 for Ivosidenib
以下数据基于产品分子量 582.96。 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 | 1.72 mL | 8.58 mL | 17.15 mL |
| 5 mM | 0.34 mL | 1.72 mL | 3.43 mL |
| 10 mM | 0.17 mL | 0.86 mL | 1.72 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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产品说明书 for Ivosidenib
参考文献 for Ivosidenib
参考文献是支持产品生物活性的出版物。
Popovici-Muller et al (2018) Discovery of AG-120 (ivosidenib): a first-in-class mutant IDH1 inhibitor for the treatment of IDH1 mutant cancers. ACS Med.Chem.Lett. 9 300 PMID: 29670690
Zarei et al (2022) Wild-type IDH1 inhibition enhances chemotherapy response in melanoma. J.Exp.Clin.Cancer Res. 41 283 PMID: 36153582
If you know of a relevant reference for Ivosidenib, please let us know.
关键词: Ivosidenib, Ivosidenib supplier, mutant, IDH1, isocitrate, dehydrogenase, potent, inhibitors, inhibits, melanoma, pancreatic, cancer, invasion, migration, Isocitrate, 1, (IDH1), 7761, 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:
- Glycolysis
- Tricarboxylic Acid Cycle
- Lipidogenesis
- 1C Metabolism and Nucleic Acid Synthesis
- Drivers of Metabolic Reprogramming
- pH and Redox Balance
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.