Cat. No.: HY-18767

Ivosidenib

(Synonyms: AG-120)

20 Cited Publications

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Based on 20 publication(s) in Google Scholar

Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity.

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Pureté: 99.89%
CAS No.: 1448347-49-6
Formule: C₂₈H₂₂ClF₃N₆O₃
Masse moléculaire:582.96

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Ivosidenib Chemical Structure

CAS No.: 1448347-49-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (20)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target

IDH1

Voir tous les produits spécifiques à Isoform Isocitrate Dehydrogenase (IDH) :

IDH1
IDH2

Cellular Effect

Cell Line	Type	Value	Description	References
HT-1080	IC₅₀	8 nM Compound: 99; AG-120	Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 37235998]
HT-1080	IC₅₀	8 nM Compound: 99; AG-120	Antiproliferative activity against human HT-1080 cells harboring IDH1 R132H mutant measured after 72 hrs by MTT assay Antiproliferative activity against human HT-1080 cells harboring IDH1 R132H mutant measured after 72 hrs by MTT assay	[PMID: 37235998]
U-87MG ATCC	IC₅₀	0.56 μM Compound: 2; AG-120	Synergistic antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs in presence of FK866 by CCK8 assay Synergistic antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs in presence of FK866 by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	0.98 μM Compound: 2; AG-120	Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	1.02 μM Compound: 2; AG-120	Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	100.06 μM Compound: 2; AG-120	Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	19 nM Compound: 99; AG-120	Antiproliferative activity against human U-87 MG cells assessed as reduction in cell growth by CCK-8 assay Antiproliferative activity against human U-87 MG cells assessed as reduction in cell growth by CCK-8 assay	[PMID: 37235998]
U-87MG ATCC	IC₅₀	19 nM Compound: 99; AG-120	Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant measured after 72 hrs by MTT assay Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant measured after 72 hrs by MTT assay	[PMID: 37235998]
U-87MG ATCC	IC₅₀	2.51 μM Compound: 2; AG-120	Synergistic antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs in presence of FK866 by CCK8 assay Synergistic antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs in presence of FK866 by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	3.06 μM Compound: 2; AG-120	Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	67.22 μM Compound: 2; AG-120	Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	89.34 μM Compound: 2; AG-120	Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 38651495]

In Vitro

Ivosidenib (AG-120) (0-13 μM; 48 hours) inhibits several IDH1-R132 mutants with potency similar IC₅₀ values: IDH1-R132H (IC₅₀=12 nM); IDH1-R132C (IC₅₀=13 nM); IDH1-R132G (IC₅₀=8 nM); IDH1-R132L (IC₅₀=13 nM); IDH1-R132S (IC₅₀=12 nM), respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AG-120 (gavage administration; 50 mg/kg and 150 mg/kg) declines tumor 2-HG concentration rapidly, with maximum inhibition (92.0% and 95.2% at the 50 mg/kg and 150 mg/kg doses, respectively) achieved at -12 h post dose^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female nude BALB/c mice inoculated with HT1080 cells^[1]
Dosage:

50 mg/kg and 150 mg/kg
Administration:

Gavage administration; 50 mg/kg and 150 mg/kg
Result:

Showed robust tumor 2-HG reduction in mouse.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1448347-49-6
Appearance Solid
Masse moléculaire 582.96
Formule C₂₈H₂₂ClF₃N₆O₃
Color White to off-white
SMILES

ClC1=C([C@H](N(C2=CC(F)=CN=C2)C([C@H]3N(C4=NC=CC(C#N)=C4)C(CC3)=O)=O)C(NC5CC(F)(F)C5)=O)C=CC=C1
Synonyms

AG-120
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (20)

All Bio/Physico-chemical AssayCell Proliferation/Viability AssayCell Imaging/Staining

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Journal Impact Factor

Imeta

2026 Feb 12.
Nat Commun

Resistance to the isocitrate dehydrogenase 1 mutant inhibitor ivosidenib can be overcome by alternative dimer-interface binding inhibitors. [Abstract]

2022 Aug 15;13(1):4785. PMID: 35970853

Ivosidenib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Aug 15;13(1):4785. [Abstract]

Inhibition (%) of IDH1 variants (400 nM) by Ivosidenib (10 µM) as determined by the NADPH absorbance assay. Errors: standard errors of the mean (n = 3 independent replicates measured on the same 96-well plate).

Ivosidenib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Aug 15;13(1):4785. [Abstract]

Non-denaturing MS analysis measuring binding of Ivosidenib to IDH1 variants. At 20 µM IDH1 variants are predominantly dimeric with 2 NADP(H) molecules bound-dashed line. Green background corresponds to binding of one Ivosidenib molecule. Final concentrations of Ivosidenib: 5 µM (4:1), 20 µM (1:1), and 160 µM (1:8). Cone-voltage: 100 V.

Ivosidenib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Aug 15;13(1):4785. [Abstract]

LN18 cells were treated with the inhibitors Ivosidenib (24 h), GSK864, FT-2102, IDH224, and DS-1001B in DMSO (final concentration: 5 µM). 2-HG levels were determined by anion-exchange chromatography coupled to MS51 (errors: standard errors of the mean, n = 4 independent replicates).
Nat Chem Biol

Autopalmitoylation of IDH1-R132H regulates its neomorphic activity in cancer cells. [Abstract]

2026 Jan 13. PMID: 41530531
Theranostics

MR-detectable metabolic biomarkers of response to mutant IDH inhibition in low-grade glioma. [Abstract]

2020 Jul 9;10(19):8757-8770. PMID: 32754276
J Exp Med

Mitochondrial metabolism supports resistance to IDH mutant inhibitors in acute myeloid leukemia. [Abstract]

2021 May 3;218(5):e20200924. PMID: 33760042
Cell Rep

Blockage of citrate export prevents TCA cycle fragmentation via Irg1 inactivation. [Abstract]

2022 Feb 15;38(7):110391. PMID: 35172156
J Med Chem

Differentiating Inhibition Selectivity and Binding Affinity of Isocitrate Dehydrogenase 1 Variant Inhibitors. [Abstract]

2023 Apr 13;66(7):5279-5288. PMID: 36952395

Ivosidenib purchased from MedChemExpress. Usage Cited in: J Med Chem. 2023 Apr 13;66(7):5279-5288. [Abstract]

Ivosidenib is the most potent IDH1 R132H inhibitor, exhibiting similar binding affinities to wild-type IDH1 and IDH1 R132H, with KD values of 416 nM and 488 nM, respectively.
Eur J Med Chem

Structure-based discovery of IHMT-IDH1-053 as a potent irreversible IDH1 mutant selective inhibitor. [Abstract]

2023 Aug 5:256:115411. PMID: 37209613
Cancer Drug Resist

Ivosidenib enhances cisplatin sensitivity in ovarian cancer by reducing cancer cell stemness. [Abstract]

2025 Apr 24:8:20. PMID: 40342735

Ivosidenib purchased from MedChemExpress. Usage Cited in: Cancer Drug Resist. 2025 Apr 24:8:20. [Abstract]

Dose-response curves of SKOV3, CAOV3, and OVCAR4 detected by MTT assay treated with cisplatin and 0 μM, 1 μM, 5 μM, 10 μM, 20 μM, and 50 μM Ivosidenib for 72 h.

Ivosidenib purchased from MedChemExpress. Usage Cited in: Cancer Drug Resist. 2025 Apr 24:8:20. [Abstract]

Quantification of cell colony number in SKOV3, CAOV3, and OVCAR4 cells treated with Ivosidenib (10 μM), Cisplatin, or their combination.
Eur J Pharm Sci

I-8, a novel inhibitor of mutant IDH1, inhibits cancer progression in vitro and in vivo. [Abstract]

2019 Dec 1;140:105072. PMID: 31518680
Drug Metab Dispos

Quantitative clinical risk assessment of CYP2C, UDP-glucuronosyltransferase, P-glycoprotein induction, and complex drug-drug interactions using TruVivo human hepatocyte triculture platform. [Abstract]

2025 Apr;53(4):100052. PMID: 40133023
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
RSC Med Chem

First-in-class small molecule inhibitors of ICOS/ICOSL interaction as a novel class of immunomodulators. [Abstract]

2023 Aug 1;14(9):1767-1777. PMID: 37731692
Cancer Res Commun

Mutant Isocitrate Dehydrogenase 1 Sensitizes Intrahepatic Cholangiocarcinoma Cells to MDM2 Inhibitors. [Abstract]

2026 Mar 1;6(3):616-629. PMID: 41747217
Front Oncol

Transcriptome Analysis of Ivosidenib-Mediated Inhibitory Functions on Non-Small Cell Lung Cancer. [Abstract]

2021 Mar 30:11:626605. PMID: 33859940
Bioorg Med Chem

Synthesis and biological evaluation of novel PET tracers [18F]AG120 & [18F]AG135 for imaging mutant isocitrate dehydrogenase 1 expression. [Abstract]

2022 Jan 1:53:116525. PMID: 34871844
Res Sq

2026 Jun 15.
bioRxiv

IDH-mutant inhibitors enhance the sensitivity of IDH1-mutant gliomas to cysteine-methionine deprivation and ferroptosis. [Abstract]

2026 Feb 2:2026.01.30.702627. PMID: 41676617
The University of Auckland

2024.
J Pers Med

Wnt/β-Catenin-Pathway Alterations and Homologous Recombination Deficiency in Cholangiocarcinoma Cell Lines and Clinical Samples: Towards Specific Vulnerabilities. [Abstract]

2022 Aug 1;12(8):1270. PMID: 36013219

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (171.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7154 mL

8.5769 mL

17.1538 mL

5 mM

0.3431 mL

1.7154 mL

3.4308 mL

10 mM

0.1715 mL

0.8577 mL

1.7154 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (8.58 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (393 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Popovici-Muller J, et al. Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1Mutant Cancers. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7154 mL	8.5769 mL	17.1538 mL	42.8846 mL
	5 mM	0.3431 mL	1.7154 mL	3.4308 mL	8.5769 mL
	10 mM	0.1715 mL	0.8577 mL	1.7154 mL	4.2885 mL
	15 mM	0.1144 mL	0.5718 mL	1.1436 mL	2.8590 mL
	20 mM	0.0858 mL	0.4288 mL	0.8577 mL	2.1442 mL
	25 mM	0.0686 mL	0.3431 mL	0.6862 mL	1.7154 mL
	30 mM	0.0572 mL	0.2859 mL	0.5718 mL	1.4295 mL
	40 mM	0.0429 mL	0.2144 mL	0.4288 mL	1.0721 mL
	50 mM	0.0343 mL	0.1715 mL	0.3431 mL	0.8577 mL
	60 mM	0.0286 mL	0.1429 mL	0.2859 mL	0.7147 mL
	80 mM	0.0214 mL	0.1072 mL	0.2144 mL	0.5361 mL
	100 mM	0.0172 mL	0.0858 mL	0.1715 mL	0.4288 mL

Keywords

Ivosidenib

20 Cited Publications

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Ivosidenib

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Publications Citing Use of MedChemExpress (MCE) Ivosidenib

Voir tous les produits spécifiques à Isoform Isocitrate Dehydrogenase (IDH)

Activité biologique

Chemical Information

Publications (20)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ivosidenib Related Classifications

Cat. No.: HY-18767