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Ivosidenib (AG-120) IDH1 inhibitor

Name: Ivosidenib (AG-120)
Brand: Selleck Chemicals
SKU: S8206
Availability: InStock
Rating: 5 (15 reviews)

Cat.No.S8206

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

Chemical Structure

Molecular Weight: 582.96

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.93%

99.93

Products Often Used Together with Ivosidenib (AG-120)

Vorasidenib (AG-881)

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

BAY 1436032

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

Olutasidenib

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

Related Targets	P450 (e.g. CYP17) PDE phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR Acyltransferase
Related Products	Glycyrrhizin (NSC 167409) Devimistat (CPI-613) Gossypol Acetate Emodin AGI-5198 AGI-6780 Sodium Dichloroacetate (DCA) NCT-503 Brequinar SW033291 RRx-001 Gossypol Farudodstat BAY 2402234 (Orludodstat) Vidofludimus Vorasidenib (AG-881) (R)-GNE-140 Merimepodib BVT 2733 AG-120 (racemic) ML390 Alda 1 Gimeracil NCT-501 G6PDi-1 Enoxolone Brequinar Sodium Alpha-Mangostin GSK 2837808A BAY 1436032

Cell Culture, Treatment & Working Concentration

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

Chemical Information, Storage & Stability

Molecular Weight	582.96	Formula	C₂₈H₂₂ClF₃N₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1448347-49-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (4.29mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	IDH1 ^[1]
In vitro	TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with Ivosidenib (AG-120). This compound decreases intracellular 2-HG levels, inhibites growth factor independent proliferation and restores erythropoietin (EPO)-induced differentiation in TF-1 IDH1-R132H cells. Similarly, its pharmacological inhibition of mutant IDH1 enzyme in primary human blast cells cultured ex vivo provides an effective way to lower intracellular 2-HG levels and induces myeloid differentiation^[1].
References	http://www.bloodjournal.org/content/124/21/3734?sso-checked=true

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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