IDH-C227, IDH1 Inhibitor


Catalog No. size PriceQuantity
M60043-2D 10 mM in DMSO (0.402 mL) $139
M60043-2S 2mg solid $139
M60043-10S 10 mg solid $549

Description

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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