Ivosidenib (AG-120)

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

Ivosidenib (AG-120) Chemical Structure

Ivosidenib (AG-120) Chemical Structure

CAS: 1448347-49-6

Selleck's Ivosidenib (AG-120) has been cited by 12 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.93%
99.93

Products often used together with Ivosidenib (AG-120)

Enasidenib (AG-221)


Ivosidenib and Enasidenib are targeted oral inhibitors of the mutant isocitrate dehydrogenase (mIDH) 1 and 2 enzymes, respectively.

Stein EM, et al . Blood. 2021;137(13):1792-1803.

Vorasidenib (AG-881)


Ivosidenib and Vorasidenib inhibit mutant forms of isocitrate dehydrogenase (mIDH) and are under clinical study for their use against mIDH glioma.

Mellinghoff IK, et al. Nat Med. 2023;29(3):615-622.

Azacitidine (5-Azacytidine)


Ivosidenib and Azacitidine use improves event-free survival and overall survival in IDH1-mutated acute myeloid leukemia.

Montesinos P, et al. N Engl J Med. 2022;386(16):1519-1531.

BAY 1436032


Ivosidenib and BAY1436032 are inhibitors of mutant isocitrate dehydrogenase 1, while Ivosidenib has been marketed and BAY1436032 is still under clinical trials.

Liu S, et al. J Med Chem. 2023 Apr 13;66(7):5279-5288.

Olutasidenib


Ivosidenib and Olutasidenib are potent and selective inhibitors of mutant IDH1 (mIDH1), which have both been marketed already.

Maschmeyer G, et al. Leukemia. 2022 May;36(5):1215-1226.

Ivosidenib (AG-120) Related Products

Choose Selective Dehydrogenase Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT1080 Function assay Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as reduction in 2-hydroxyglutarate production, IC50 = 0.0075 μM. 29079473
Click to View More Cell Line Experimental Data

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
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 Research 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.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06127407 Not yet recruiting
Locally Advanced or Metastatic Conventional Chondrosarcoma With an IDH1 Mutation Untreated or Previously Treated With 1 Systemic Treatment Regimen
Servier Bio-Innovation LLC|Institut de Recherches Internationales Servier|Servier
April 1 2024 Phase 3
NCT06181734 Recruiting
Acute Myeloid Leukemia (AML)
iOMEDICO AG
January 2024 --
NCT05907057 Recruiting
Acute Myeloid Leukemia (AML)
Servier Affaires Médicales|Servier
June 14 2023 Phase 3
NCT04955938 Recruiting
IDH Mutation|IDH1 Mutation|IDH2 Gene Mutation|Blood Cancer|Myeloproliferative Neoplasm
University of Chicago
October 29 2021 Phase 1
NCT04195555 Active not recruiting
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 2 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 2 Glioma|Wilms Tumor
National Cancer Institute (NCI)|Children''s Oncology Group
July 20 2020 Phase 2

Chemical Information & Solubility

Molecular Weight 582.96 Formula

C28H22ClF3N6O3

CAS No. 1448347-49-6 SDF Download Ivosidenib (AG-120) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (171.53 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Ivosidenib (AG-120) | Ivosidenib (AG-120) supplier | purchase Ivosidenib (AG-120) | Ivosidenib (AG-120) cost | Ivosidenib (AG-120) manufacturer | order Ivosidenib (AG-120) | Ivosidenib (AG-120) distributor