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Mutant IDH1-IN-6

Catalog No. T39716 CAS 2230263-60-0

Synonyms: Mutant IDH1-IN-6

Mutant IDH1-IN-6 is an orally active compound that effectively inhibits mutant isocitrate dehydrogenase (IDH) enzymes. It demonstrates potency and selectivity, with IC50 values of 6.27, 3.71, 36.9, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutants, respectively. Notably, Mutant IDH1-IN-6 exhibits lower activity in inhibiting wild-type IDH enzymes.

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Mutant IDH1-IN-6, CAS 2230263-60-0

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Description	Mutant IDH1-IN-6 is an orally active compound that effectively inhibits mutant isocitrate dehydrogenase (IDH) enzymes. It demonstrates potency and selectivity, with IC50 values of 6.27, 3.71, 36.9, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutants, respectively. Notably, Mutant IDH1-IN-6 exhibits lower activity in inhibiting wild-type IDH enzymes.
Targets&IC50	IDH2 (R172K):11.5 nM (IC50), IDH1 (R132C):3.71 nM (IC50), IDH2 (R140Q):36.9 nM (IC50), IDH1 (R132H):6.27 nM (IC50), IDH2 (WT):884 nM (IC50), IDH1 (WT):105 nM (IC50)
In vitro	Mutant IDH1-IN-6 (example 2) selectively inhibits the production of 2-hydroxyglutarate in HT1080 cells, targeting the mutant IDH1 R132C with an IC50 of 1.28 nM without affecting aKG production, a metabolite from wild-type IDH1. This specificity indicates the compound's selectivity for mutant over wild-type IDH1 in cellular environments[1].
In vivo	Treatment with Mutant IDH1-IN-6 (Example 2; 0-32 mg/kg; oral gavage; twice daily for 3 days) hampers the production of 2-hydroxyglutarate in a dose-responsive manner in IDH1 mutant xenograft mice [1]. The study utilized athymic nude mice (20-22 g), which were administered TB08 cells, exploring dosage levels ranging from 1 mg/kg to 32 mg/kg. The regimen involved oral gavage administered twice daily over a period of three days, resulting in the inhibition of 2-hydroxyglutarate in IDH1 mutant xenograft mice.

Synonyms	Mutant IDH1-IN-6
Molecular Weight	504.635
Formula	C28H36N6O3
CAS No.	2230263-60-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Renato Alejandro BAUER, et al. 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitors. WO2018111707A1.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Mutant IDH1-IN-6 2230263-60-0 Mutant IDH1 IN 6 Mutant IDH-1-IN-6 Mutant IDH1IN6 inhibitor inhibit

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