Vorasidenib (AG-881)

For research use only.

Catalog No.S8611

2 publications

Vorasidenib (AG-881) Chemical Structure

CAS No. 1644545-52-7

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

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Selleck's Vorasidenib (AG-881) has been cited by 2 publications

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Biological Activity

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


Solubility (25°C)

In vitro DMSO 82 mg/mL (197.71 mM)
Ethanol 82 mg/mL (197.71 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 414.74


CAS No. 1644545-52-7
Storage powder
in solvent
Synonyms N/A
Smiles CC(C(F)(F)F)NC1=NC(=NC(=N1)C2=NC(=CC=C2)Cl)NC(C)C(F)(F)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04164901 Recruiting Drug: AG-881|Drug: Matching Placebo Grade 2 Glioma|Residual Glioma|Recurrent Glioma Agios Pharmaceuticals Inc. January 5 2020 Phase 3
NCT04145128 Completed Drug: AG881 Healthy Volunteers Agios Pharmaceuticals Inc. October 2 2019 Phase 1
NCT04015687 Completed Drug: AG-881|Drug: Lamotrigine Healthy Participants Agios Pharmaceuticals Inc. July 15 2019 Phase 1
NCT03960502 Completed Drug: AG-881|Drug: [13C315N3]AG-881 Healthy Male Participants Agios Pharmaceuticals Inc. May 16 2019 Phase 1
NCT03343197 Active not recruiting Drug: AG-120|Drug: AG881 Glioma Agios Pharmaceuticals Inc. March 20 2018 Phase 1

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