Ivosidenib (AG-120)

Catalog No.S8206

For research use only.

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

Ivosidenib (AG-120) Chemical Structure

CAS No. 1448347-49-6

Selleck's Ivosidenib (AG-120) has been cited by 6 Publications

2 Customer Reviews

Purity & Quality Control

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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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT1080 NIDSXW5HfW6ldHnvckBie3OjeR?= NHvGelRKdmirYnn0bY9vKG:oIFnETFEhWjF|MlOgcZV1[W62IHnuJIh2dWGwIFjUNVA5OCClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gNk1pgWS{b4j5[4x2fGG{YYTlJJBzd2S3Y4Tpc44tKEmFNUCgQUAxNjByN{Wg{txONg>? M124WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MEe5OFc{Lz5{OUC3PVQ4OzxxYU6=

Protocol (from reference)

Cell Research:

[1]

  • 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.

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(171.53 mM)
Ethanol 100 mg/mL
(171.53 mM)
Water Insoluble

Chemical Information

Molecular Weight 582.96
Formula

C28H22ClF3N6O3

CAS No. 1448347-49-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(=O)N(C1C(=O)N(C2=CC(=CN=C2)F)C(C3=CC=CC=C3Cl)C(=O)NC4CC(C4)(F)F)C5=NC=CC(=C5)C#N

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04955938 Recruiting Drug: Ivosidenib|Drug: Enasidenib|Drug: Fedratinib IDH Mutation|IDH1 Mutation|IDH2 Gene Mutation|Blood Cancer|Myeloproliferative Neoplasm University of Chicago October 29 2021 Phase 1
NCT04195555 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)|Children''s Oncology Group June 8 2020 Phase 2
NCT03564821 Active not 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 Institut de Recherches Internationales Servier|Servier March 20 2018 Phase 1
NCT02831972 Completed Drug: AG120|Drug: Itraconazole Healthy Agios Pharmaceuticals Inc. June 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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