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Mutant IDH1-IN-1

Names

[ CAS No. ]:
1355326-21-4

[ Name ]:
Mutant IDH1-IN-1

[Synonym ]:
2-(1H-Benzimidazol-1-yl)-N-[2-(cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)acetamide
1H-Benzimidazole-1-acetamide, N-[2-(cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-
Mutant IDH1-IN-1

Biological Activity

[Description]:

Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Isocitrate Dehydrogenase (IDH)
Research Areas >> Cancer

[Target]

IC50: 4 nM (IDH1 R132C/R132C), 42 nM (IDH1 R132H/R132H), 80 nM (IDH1 R132H/WT), 143 nM (IDH1 wild type)[1]


[References]

[1]. Deng G, et al. Selective inhibition of mutant isocitrate dehydrogenase 1 (IDH1) via disruption of a metal binding network by an allosteric small molecule. J Biol Chem. 2015 Jan 9;290(2):762-74.


[Related Small Molecules]

AG-120 | Enasidenib | AGI-5198 | Vorasidenib (AG-881) | AGI-6780 | GSK864 | IDH-305 | BAY-1436032 | Mutant IDH1 inhibitor | Mutant IDH1-IN-2 | Olutasidenib

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Molecular Formula ]:
C30H31FN4O2

[ Molecular Weight ]:
498.591

[ Exact Mass ]:
498.243103

[ LogP ]:
5.62

[ Index of Refraction ]:
1.637

[ Storage condition ]:
2-8℃

Related Compounds