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IDH1 Inhibitor 1

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IDH1 Inhibitor 1

Catalog No. T11613Cas No. 2234285-81-3

IDH1 Inhibitor 1 is an orally bioavailable, brain-penetrant, and selective mutant IDH1 inhibitor (IC50s: 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT).

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Pack Size	Price	Availability
25 mg	$2,270	10-14 weeks
50 mg	$2,980	10-14 weeks
100 mg	$4,000	10-14 weeks

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Product Introduction

Bioactivity

Description	IDH1 Inhibitor 1 is an orally bioavailable, brain-penetrant, and selective mutant IDH1 inhibitor (IC50s: 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT).
Targets&IC50	IDH1 (R132H):0.021 μM , IDH1 (WT):2.52 μM , IDH1 (R132C):0.045 μM
In vitro	IDH1 Inhibitor 1 inhibits cellular HCT116-IDH1R132H/+ with an IC50 of 0.039 μM.
In vivo	IDH1 Inhibitor 1 is also profiled in a patient-derived IDH1 mutant HCT116-IDH1R132H/+ mechanistic xenograft tumor model in mice to evaluate in vivo inhibition of 2-HG production. IDH1 Inhibitor 1, dosed orally at 150 mg/kg, inhibits new 2-HG production.IDH1 Inhibitor 1 ?inhibits 2-hydroxyglutarate (2-HG) production in a preclinical xenograft tumor model.

Chemical Properties

Molecular Weight	450.39
Formula	C20H18F4N6O2
Cas No.	2234285-81-3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

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Keywords

IDH-1 Inhibitor 1IDH1 Inhibitor 1