Ivosidenib (AG-120)

For research use only.

Catalog No.S8206

3 publications

Ivosidenib (AG-120) Chemical Structure

Molecular Weight(MW): 582.96

Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.

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Selleck's Ivosidenib (AG-120) has been cited by 3 publications

2 Customer Reviews

  • (C) MGC-803 cells were treated with the control (DMEM culture), 1% alcohol (DMEM culture medium with 1% alcohol) and AG-120 (40, 60, 80 and 100 µM) for 24, 48 or 72 h.

    Oncol Rep, 2017, 38(6):3583-3591. Ivosidenib (AG-120) purchased from Selleck.

    MGC-803 cells were treated with the control (DMEM culture), 1% alcohol (DMEM culture medium with 1% alcohol) and AG-120 (40, 60, 80 and 100 μM) for 24, 48 or 72 h. The MTT assay was performed to determine cell viability and values are expressed as the mean ± SD of three separate experiments. *p<0.05 vs. control.

    ONCOLOGY REPORTS, 2017, 38: 3583-3591. Ivosidenib (AG-120) purchased from Selleck.

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Biological Activity

Description Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.
Targets
IDH1 [1]
In vitro

TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120.Treatment with AG-120 decreases intracellular 2-HG levels, inhibites growth factor independent proliferation and restores erythropoietin (EPO)-induced differentiation in TF-1 IDH1-R132H cells. Similarly, pharmacological inhibition of mutant IDH1 enzyme with AG-120 in primary human blast cells cultured ex vivo provides an effective way to lower intracellular 2-HG levels and induces myeloid differentiation[1].

Protocol

Cell Research:

[1]

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  • Cell lines: TF-1 cells
  • Concentrations: 0.5, 1.0, and 5.0 μM
  • Incubation Time: 6 days
  • Method:

    TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (171.53 mM)
Ethanol 100 mg/mL (171.53 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 582.96
Formula

C28H22ClF3N6O3

CAS No. 1448347-49-6
Storage powder
in solvent
Synonyms
Smiles FC1=CN=CC(=C1)N(C(C(=O)NC2CC(F)(F)C2)C3=C(Cl)C=CC=C3)C(=O)C4CCC(=O)N4C5=NC=CC(=C5)C#N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04195555 Not yet recruiting Drug: Ivosidenib Recurrent Ependymoma|Recurrent Ewing Sarcoma|Recurrent Hepatoblastoma|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Glioma|Recurrent Malignant Solid Neoplasm|Recurrent Medulloblastoma|Recurrent Neuroblastoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Rhabdoid Tumor|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Recurrent WHO Grade II Glioma|Refractory Ependymoma|Refractory Ewing Sarcoma|Refractory Hepatoblastoma|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Germ Cell Tumor|Refractory Malignant Glioma|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Refractory WHO Grade II Glioma|Wilms Tumor National Cancer Institute (NCI) September 6 2020 Phase 2
NCT03564821 Recruiting Drug: Ivosidenib IDH1 Mutation Myeloid Neoplasms Massachusetts General Hospital|Agios Pharmaceuticals Inc. January 16 2019 Phase 1
NCT03343197 Active not recruiting Drug: AG-120|Drug: AG881 Glioma Agios Pharmaceuticals Inc. March 20 2018 Phase 1
NCT02831972 Completed Drug: AG120|Drug: Itraconazole Healthy Agios Pharmaceuticals Inc. June 2016 Phase 1
NCT02489513 Completed Drug: [14C]-AG-120 Healthy Volunteers Agios Pharmaceuticals Inc. June 2015 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID