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Mutant IDH1-IN-1

  Cat. No.:  DC7982   Featured
Chemical Structure
1355326-21-4
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More than 5000 active chemicals with high quality for research!
Field of application
Mutant IDH1-IN-1 is a potent mutant IDH1 R132H inhibitor with IC50 < 0.1 uM(A level in Patent).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1355326-21-4
SMILES: CC1=CC=CC=C1C(N(C(CN2C=NC3=CC=CC=C32)=O)C4=CC=CC(F)=C4)/C(O)=N/C5CCCCC5
Formula: C30H31FN4O2
M.Wt: 498.59
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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.
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC7982 Mutant IDH1-IN-1 Mutant IDH1-IN-1 is a potent mutant IDH1 R132H inhibitor with IC50 < 0.1 uM(A level in Patent).
DC10830 IDH-889 IDH889 is a potent and selective inhibitors of IDH1. IDH899 shows IDH (R132H) IC50 = 20 nM; Cell 2-HG IC50 = 14 nM.
DC10538 IDH-305 IDH305 is an inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity.
DC7174 AGI-6780 AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q (IC50=23 nM).
DC5050 AGI-5198 AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.
DC10439 Vorasidenib (AG881) AG-881 is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1) in the cytoplasm and type 2 (IDH2).
DC8374 AG-221(Enasidenib) AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein.
DC8051 AG-120 (Ivosidenib) AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.
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