产品详情
简单介绍：
IDH-C227,IDH1Inhibitor
详情介绍：
Product Information
| Molecular Weight: | 498.59 |
| Formula: | C30H31FN4O2 |
| Purity: | ≥98% |
| CAS#: | 1355324-14-9 |
| Solubility: | DMSO up to 50 mM |
| Chemical Name: | 2-((4-cyanophenyl)amino)-N-(2-(cyclohexylamino)-2-oxo-1-(o-tolyl)ethyl)-N-(3-fluorophenyl)acetamide |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
IDH-C227 is a potent and selective IDH1 R132H inhibitor first reported in patent WO2012009678. It can inhibit the enzymatic activity of IDH1 R132H in vitro with an IC50 < 0.1 µM, and 2-HG production in HT1080 and U87MG cells with IC50 < 0.25 µM. Because the mutated form of IDH1 produces the metabolite, 2-hydroxyglutarate (2HG), which may contribute to the formation and malignant progression of gliomas as well as other forms of cancer, IDH-C227 serves as a very useful chemical probe to study this novel target.
How to Use:
- In vitro: IDH-C227 was used at 1-5 µM final concentration in vitro.
- In vivo: n/a. You can try the new generation IDH1 inhibitor IDH-C35 for in vivo use.
Reference:
- 1. Popovicimuller Janeta, et al. THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHOD OF USE. (2012) PCT WO 2012009678.
- 2. Dang L, et al. Cancer-associated IDH1 mutations produce 2-hydroxyglutarate. (2009) Nature 462, 739-744.
- 3. Turcan S, et al. IDH1 mutation is sufficient to establish the glioma hypermethylator phenotype. (2012) Nature. 483(7390):479-83.
Products are for research use only. Not for human use.
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