Choose Your Country or Region

Ivosidenib (AG-120)

Name: Ivosidenib (AG-120)
Brand: Selleck Chemicals
SKU: S8206
Rating: 5 (12 reviews)

Catalog No.S8206 Purity: 99.93%

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

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.

Other Dehydrogenase Products

Related compound libraries

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

[1] Erica Hansen, et al. Blood. 2104, 124:3734.

Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
=	×	×

Dilution Calculator Molecular Weight Calculator

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.

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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):