Home Metabolism Dehydrogenase inhibitor Ivosidenib (AG-120) For research use only.

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 No. 1448347-49-6

Ivosidenib (AG-120) Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

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
 June 7 2024 Phase 3
NCT06377579 Not yet recruiting
AML Adult
French Innovative Leukemia Organisation|Acute Leukemia French Association
 May 15 2024 --
NCT06181734 Recruiting
Acute Myeloid Leukemia (AML)
iOMEDICO AG
 December 20 2023 --
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

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)

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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

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