Description
IDH-C227, CAS No. 1355324-14-9, 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.
Product information
CAS Number: 1355324-14-9
Molecular Weight: 498.59
Formula: C30H31FN4O2
Chemical Name: 2-((4-cyanophenyl)amino)-N-(2-(cyclohexylamino)-2-oxo-1-(o-tolyl)ethyl)-N-(3-fluorophenyl)acetamide
Smiles: CC1=CC=CC=C1C(C(=O)NC1CCCCC1)N(C1=CC(F)=CC=C1)C(=O)CNC1C=CC(=CC=1)C#N
InChiKey: AATMNHPDEZNXEK-UHFFFAOYSA-N
InChi: InChI=1S/C30H31FN4O2/c1-21-8-5-6-13-27(21)29(30(37)34-25-10-3-2-4-11-25)35(26-12-7-9-23(31)18-26)28(36)20-33-24-16-14-22(19-32)15-17-24/h5-9,12-18,25,29,33H,2-4,10-11,20H2,1H3,(H,34,37)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
IDH-C227 was used at 1-5 µM final concentration in vitro.
In Vivo:
n/a (try to use IDH-C35 for in vivo studies)
References:
- Popovicimuller Janeta, et al. THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHOD OF USE. (2012) PCT WO 2012009678.
- Dang L, et al. Cancer-associated IDH1 mutations produce 2-hydroxyglutarate. (2009) Nature 462, 739-744.
- 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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