Vorasidenib (AG-881)

For research use only.

Catalog No.S8611

2 publications

Vorasidenib (AG-881) Chemical Structure

Molecular Weight(MW): 414.74

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).
Targets
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].

Protocol

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
Formula

C14H13ClF6N6

CAS No. 1644545-52-7
Storage powder
in solvent
Synonyms N/A
Smiles CC(NC1=NC(=NC(=N1)C2=CC=CC(=N2)Cl)NC(C)C(F)(F)F)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

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.

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Dehydrogenase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID