Home Metabolism Dehydrogenase inhibitor Vorasidenib (AG-881) For research use only.

Vorasidenib (AG-881)

Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2).

Vorasidenib (AG-881) Chemical Structure

Vorasidenib (AG-881) Chemical Structure

CAS No. 1644545-52-7

Purity & Quality Control

Vorasidenib (AG-881) Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87MG Antiproliferative assay 72 hrs Antiproliferative activity against human U87MG cells expressing pLVX-IDH2 R140Q mutant after 72 hrs by celltiterglo reagent based assay, IC50<0.05μM 29847930
TS603 Antiproliferative assay 72 hrs Antiproliferative activity against human TS603 cells harboring IDH2 R140Q mutant after 72 hrs by celltiterglo reagent based assay, IC50<0.05μM 29847930
HT1080 Antiproliferative assay 72 hrs Antiproliferative activity against human HT1080 cells after 72 hrs by celltiterglo reagent based assay, IC50<0.05μM 29847930
Sf9 Function assay 1 hr Inhibition of His-tagged wild type IDH1 (unknown origin)/FLAG-tagged IDH1 R132H mutant heterodimer expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by diaphorase and resazurin addition and measured after 5 mins in presenc, IC50<0.05μM ChEMBL
Sf9 Function assay 1 hr Inhibition of His-tagged wild type IDH1 (unknown origin)/FLAG-tagged IDH1 R132C mutant heterodimer expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by diaphorase and resazurin addition and measured after 5 mins in presenc, IC50<0.05μM ChEMBL
Sf9 Function assay 1 hr Inhibition of DH1 R132H mutant homodimer (unknown origin) expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by 60 mins incubation in presence of NADPH, NADP, diaphorase and resazurin by fluorescence spectrometry, IC50<0.05μM ChEMBL
Sf9 Function assay 1 hr Inhibition of DH1 R132C mutant homodimer (unknown origin) expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by 60 mins incubation in presence of NADPH, NADP, diaphorase and resazurin by fluorescence spectrometry, IC50<0.05μM ChEMBL
Sf9 Function assay 1 hr Inhibition of IDH2 R140Q mutant homodimer (unknown origin) expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by 16 hrs incubation in presence of NADPH, NADP, diaphorase and resazurin by fluorescence spectrometry based cofa, IC50<0.05μM ChEMBL
HT1080 Function assay 48 hrs Inhibition of IDH1 R132H/R132C mutant in human HT1080 cells assessed as reduction in 2-HG formation incubated for 48 hrs by LC-MS method, IC50<0.05μM ChEMBL
U87MG Function assay 48 hrs Inhibition of IDH1 R132C mutant (unknown origin) expressed in human U87MG cells assessed as reduction in 2-HG formation incubated for 48 hrs by LC-MS method, IC50<0.05μM ChEMBL
TS603 Function assay 48 hrs Inhibition of DH1 R132H mutant in human TS603 cells assessed as reduction in 2-HG formation incubated for 48 hrs by LC-MS method, IC50<0.05μM ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2).
Targets
IDH1 [1] IDH2 [1]
In vitro
In vitro Pan-IDH1/2 inhibitor (AG881) selectively inhibit mutant IDH protein and induce cell differentiation in in vitro and in vivo models[1]. Upon administration, pan-IDH mutant inhibitor AG-881 specifically inhibits mutant forms of IDH1 and IDH2, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH mutations[2].
In Vivo
In vivo AG-881 fully penetrates the blood-brain barrier. AG-881 has been developed and is in early phase I testing for patients with IDH mutation-positive hematologic malignancies and solid tumors, including glioma[3].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05609994 Not yet recruiting
Low Grade Glioma of Brain
Katy Peters MD PhD|Servier|Duke University
 June 2024 Phase 1
NCT05674474 Completed
Hepatic Impairment
Institut de Recherches Internationales Servier|Servier
 March 14 2023 Phase 1
NCT05484622 Recruiting
Astrocytoma
Institut de Recherches Internationales Servier|Merck Sharp & Dohme LLC|Servier
 January 20 2023 Phase 1
NCT04145128 Completed
Healthy Volunteers
Agios Pharmaceuticals Inc.
 October 2 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 414.74 Formula

C14H13ClF6N6
CAS No. 1644545-52-7 SDF Download Vorasidenib (AG-881) SDF
Smiles CC(C(F)(F)F)NC1=NC(=NC(=N1)C2=NC(=CC=C2)Cl)NC(C)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 82 mg/mL ( (197.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 82 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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