AGI-5198
Based on 20 publication(s) in Google Scholar
AGI-5198 (IDH-C35) is a potent and selective mutant IDH1R132H inhibitor with an IC50 of 0.07 μM.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 1355326-35-0
- Formula: C27H31FN4O2
- Molecular Weight:462.56
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AGI-5198
More- Nat Cell Biol. 2024 Jun;26(6):1003-1018. [Abstract]
- Cancer Res. 2018 Nov 15;78(22):6386-6398. [Abstract]
- Cancer Res. 2015 Nov 15;75(22):4790-802. [Abstract]
- Nat Commun. 2025 Jul 26;16(1):6913. [Abstract]
- Nat Commun. 2025 Apr 24;16(1):3874. [Abstract]
- Nat Chem Biol. 2026 Jan 13. [Abstract]
- Clin Cancer Res. 2024 Sep 13;30(18):4068-4076. [Abstract]
- Clin Cancer Res. 2024 May 8. [Abstract]
- Clin Cancer Res. 2018 Apr 1;24(7):1705-1715. [Abstract]
- J Med Chem. 2023 Apr 13;66(7):5279-5288. [Abstract]
- Cancer Metab. 2019 May 20:7:4. [Abstract]
- Cancers (Basel). 2022 Dec 17;14(24):6228. [Abstract]
- FASEB J. 2018 Jun 7;32(11):fj201800547R. [Abstract]
- Neurooncol Adv. 2026 Mar 2.
- ACS Med Chem Lett. 2015 Jun 22;6(8):948-52. [Abstract]
- Mol Carcinog. 2025 Apr;64(4):652-667. [Abstract]
- J Neurooncol. 2018 Jun;138(2):241-250. [Abstract]
- PLoS One. 2020 Sep 18;15(9):e0239325. [Abstract]
- Research Square Preprint. 2024 Apr 19.
- Oncotarget. 2017 Jul 25;8(30):49165-49177. [Abstract]
Customer Validation & Images
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IF
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Biological Activity
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IDH1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | EC50 |
>50 μM
Compound: 1, AGI-5198
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Cytotoxicity against human A549 cells assessed as growth inhibition after 48 to 96 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as growth inhibition after 48 to 96 hrs by MTT assay
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[PMID: 26280302] |
| HT-1080 | EC50 |
>50 μM
Compound: 1, AGI-5198
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Cytotoxicity against human HT1080 cells assessed as growth inhibition after 48 to 96 hrs by MTT assay
Cytotoxicity against human HT1080 cells assessed as growth inhibition after 48 to 96 hrs by MTT assay
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[PMID: 26280302] |
| HT-1080 | GI50 |
>20 μM
Compound: 35
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Growth inhibition of human HT1080 cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of human HT1080 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 24900389] |
| HT-1080 | IC50 |
<0.25 μM
Compound: 1; AGI-5198
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Inhibition of IDH1 R132H mutant in human HT-1080 cells assessed as suppression of 2-HG production incubated for 48 hrs by LC-MS analysis
Inhibition of IDH1 R132H mutant in human HT-1080 cells assessed as suppression of 2-HG production incubated for 48 hrs by LC-MS analysis
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[PMID: 29847930] |
| HT-1080 | IC50 |
0.48 μM
Compound: 35
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Inhibition of IDH1 R132C mutant overexpressed in human HT1080 cells assessed as inhibition of 2-hydroxyglutarate production after 48 hrs by LC/MS analysis
Inhibition of IDH1 R132C mutant overexpressed in human HT1080 cells assessed as inhibition of 2-hydroxyglutarate production after 48 hrs by LC/MS analysis
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[PMID: 24900389] |
| MCF7 | EC50 |
>50 μM
Compound: 1, AGI-5198
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Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 to 96 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 to 96 hrs by MTT assay
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[PMID: 26280302] |
| U-87MG ATCC | GI50 |
>20 μM
Compound: 35
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Growth inhibition of human U87 cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of human U87 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 24900389] |
| U-87MG ATCC | IC50 |
0.07 μM
Compound: 35
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Inhibition of IDH1 R132H mutant expressed in human U87 cells assessed as inhibition of 2-hydroxyglutarate production after 48 hrs by LC/MS analysis
Inhibition of IDH1 R132H mutant expressed in human U87 cells assessed as inhibition of 2-hydroxyglutarate production after 48 hrs by LC/MS analysis
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[PMID: 24900389] |
| U-87MG ATCC | IC50 |
20.1 μM
Compound: AGI-5198
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Antiproliferative activity against human U87 cells by MTT assay
Antiproliferative activity against human U87 cells by MTT assay
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[PMID: 30108937] |
| WI-38 | EC50 |
>50 μM
Compound: 1
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Inhibition of cell proliferation of human WI38 cells by CCK8 assay
Inhibition of cell proliferation of human WI38 cells by CCK8 assay
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[PMID: 25271760] |
| WI-38 | EC50 |
>50 μM
Compound: 1, AGI-5198
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Cytotoxicity against human WI38 cells assessed as growth inhibition after 48 to 96 hrs by MTT assay
Cytotoxicity against human WI38 cells assessed as growth inhibition after 48 to 96 hrs by MTT assay
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[PMID: 26280302] |
Measurements of R-2HG concentrations in pellets of TS603 glioma cells demonstrates dose-dependent inhibition of the mutant IDH1 enzyme by AGI-5198. AGI-5198 does not impair colony formation of two patient-derived glioma lines that express only the wild-type IDH1 allele (TS676 and TS516)[1]. Cancer cells heterozygous for the IDH1(R132H) mutation exhibits less IDH-mediated production of NADPH, such that after exposure to ionizing radiation (IR), there are higher levels of reactive oxygen species, DNA double-strand breaks, and cell death compared with IDH1 wild-type cells. These effects are reversed by the IDH1(R132H) inhibitor AGI-5198[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1355326-35-0
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Appearance Solid
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Molecular Weight 462.56
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Formula C27H31FN4O2
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Color White to off-white
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SMILES
FC1=CC=CC(N(C(C2=CC=CC=C2C)C(NC3CCCCC3)=O)C(CN4C=CN=C4C)=O)=C1
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Synonyms
IDH-C35
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (20)
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Journal Impact Factor
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Most Recent
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Nat Cell Biol
Tumour microenvironment programming by an RNA-RNA-binding protein complex creates a druggable vulnerability in IDH-wild-type glioblastoma. [Abstract]2024 Jun;26(6):1003-1018. PMID: 38858501 -
Cancer Res
2018 Nov 15;78(22):6386-6398. PMID: 30254149
AGI-5198 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2018 Nov 15;78(22):6386-6398. [Abstract]
IDH1R132H-mediated epigenetic silencing of TSGs is inhibited by cyclin F.
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Cancer Res
2015 Nov 15;75(22):4790-802. PMID: 26363012 -
Nat Commun
A genetically encoded biosensor for point-of-care and live-cell detection of D-2-hydroxyglutarate. [Abstract]2025 Jul 26;16(1):6913. PMID: 40715112 -
Nat Commun
2025 Apr 24;16(1):3874. PMID: 40274791 -
Nat Chem Biol
2026 Jan 13. PMID: 41530531 -
Clin Cancer Res
2024 Sep 13;30(18):4068-4076. PMID: 39042445 -
Clin Cancer Res
2024 May 8. PMID: 38718141 -
Clin Cancer Res
IDH1/2 Mutations Sensitize Acute Myeloid Leukemia to PARP Inhibition and This Is Reversed by IDH1/2-Mutant Inhibitors. [Abstract]2018 Apr 1;24(7):1705-1715. PMID: 29339439 -
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 -
Cancer Metab
Isocitrate dehydrogenase 1-mutated cancers are sensitive to the green tea polyphenol epigallocatechin-3-gallate. [Abstract]2019 May 20:7:4. PMID: 31139406 -
Cancers (Basel)
Hyperthermia as a Potential Cornerstone of Effective Multimodality Treatment with Radiotherapy, Cisplatin and PARP Inhibitor in IDH1-Mutated Cancer Cells. [Abstract]2022 Dec 17;14(24):6228. PMID: 36551714 -
FASEB J
IDH1-mutant cancer cells are sensitive to cisplatin and an IDH1-mutant inhibitor counteracts this sensitivity. [Abstract]2018 Jun 7;32(11):fj201800547R. PMID: 29879375
AGI-5198 purchased from MedChemExpress. Usage Cited in: FASEB J. 2018 Jun 7;32(11):fj201800547R. [Abstract]
Representative photomicrographs of cells that are plated on glass coverslips in the presence or absence of 1μM AGI-5198, treated with 5 or 10μM Cisplatin for 1 h, and fixed after 30 min. γ-H2AX is stained immunocytochemically (red) to demonstrate DNA DSBs and with DAPI (blue) to demonstrate DNA nucleus content.
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ACS Med Chem Lett
High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. [Abstract]2015 Jun 22;6(8):948-52. PMID: 26288699 -
Mol Carcinog
RNF7-Mediated ROS Targets Malignant Phenotype and Radiotherapy Sensitivity in Glioma With Different IDH1 Genotypes. [Abstract]2025 Apr;64(4):652-667. PMID: 39783768 -
J Neurooncol
2018 Jun;138(2):241-250. PMID: 29453678
AGI-5198 purchased from MedChemExpress. Usage Cited in: J Neurooncol. 2018 Jun;138(2):241-250. [Abstract]
LN18 IDH1 R132H cells are either treated with vehicle (DMSO) or 1 μM AG-5198 for the indicated number of days. Cells are harvested and Fn14, PAR-4 and GAPDH levels are evaluated by Western blot analysis.
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PLoS One
Generation of induced neural stem cells with inducible IDH1R132H for analysis of glioma development and drug testing. [Abstract]2020 Sep 18;15(9):e0239325. PMID: 32946483 -
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Oncotarget
In silico gene expression analysis reveals glycolysis and acetate anaplerosis in IDH1 wild-type glioma and lactate and glutamate anaplerosis in IDH1-mutated glioma. [Abstract]2017 Jul 25;8(30):49165-49177. PMID: 28467784
Solvent & Solubility
DMF : ≥ 50 mg/mL (108.09 mM)
DMSO : 20.83 mg/mL (45.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.50 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Inhibitory potency against the IDH2 R140Q and IDH2 R172K enzymes is determined in an endpoint assay in which the amount of NADPH remaining at the end of the reaction is measured by the addition of a large excess of diaphorase and resazurin. IDH2 R140Q is diluted to 0.25 μg/mL in 40 μL 1X Assay Buffer (150 mM NaCl, 50 mM potassium phosphate pH 7.5, 10 mM MgCl2, 10% glycerol, 2 mM B-ME, 0.03% BSA) and incubated for 16 hours at 25°C in the presence of 1 μL of compound in DMSO. The reaction is started with the addition of 10 μL of Substrate Mix (20 μM NADPH, 8 μM alpha-ketoglutarate, in 1X Assay Buffer) and incubated for 1 hour at 25°C. Then, remaining NADPH is measured by the addition of 25 μL of Detection Mix (36 μg/mL diaphorase, 18 μM resazurin in 1X Assay buffer), incubated for 5 minutes at 25°C, and read as described above. IDH2 R172K is assayed as for IDH2 R140Q with the following modifications: 1.25 μg/mL of protein is used, the Substrate Mix contained 50 μM NADPH and 6.4 μM alpha-ketoglutarate, and the compound is incubated for 1 hour before starting the reaction.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TS603 cells are grown in medium containing either AGI-5198 (1.5μM) or DMSO vehicle control. One week prior to harvest cells are ransferred to differentiation medium (DMEM F12; 15 mM HEPES; 0.06% glucose; B27 without vitamin A; N2; Insulin/transferrin; 1% FBS) containing freshly added retinoic acid (1μM). ChIP of non-crosslinked cells is then carried out using established ChIP methods. 350 μg of lysate is immunoprecipitated-using anti-H3K9Me3, H3K27me3 or Rabbit Control IgG. After washing, ChIP DNA is eluted from protein G beads and analyzed by RT-PCR using SYBR green. Relative occupancy is calculated using the standard curve method and fold enrichment versus IgG. Enrichment in AGI- 5198-treated cells is normalized to vehicle control. Means and standard deviation are calculated from 4 technical replicates.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SCID mice are injected subcutaneously with 106 glioma cells, which are suspended in 100 μL of a 50:50 mixture of growth media and Matrigel. Once tumors have reached a measurable size, mice are randomized into the indicated treatment groups.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Rohle D, et al. An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells. Science. 2013 May 3;340(6132):626-30. [Content Brief]
[2]. Molenaar RJ, et al. Radioprotection of IDH1-Mutated Cancer Cells by the IDH1-Mutant Inhibitor AGI-5198. Cancer Res. 2015 Nov 15;75(22):4790-802. [Content Brief]
Complete Stock Solution Preparation Table
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / DMF | 1 mM | 2.1619 mL | 10.8094 mL | 21.6188 mL | 54.0470 mL |
| 5 mM | 0.4324 mL | 2.1619 mL | 4.3238 mL | 10.8094 mL | |
| 10 mM | 0.2162 mL | 1.0809 mL | 2.1619 mL | 5.4047 mL | |
| 15 mM | 0.1441 mL | 0.7206 mL | 1.4413 mL | 3.6031 mL | |
| 20 mM | 0.1081 mL | 0.5405 mL | 1.0809 mL | 2.7024 mL | |
| 25 mM | 0.0865 mL | 0.4324 mL | 0.8648 mL | 2.1619 mL | |
| 30 mM | 0.0721 mL | 0.3603 mL | 0.7206 mL | 1.8016 mL | |
| 40 mM | 0.0540 mL | 0.2702 mL | 0.5405 mL | 1.3512 mL | |
| DMF | 50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0809 mL |
| 60 mM | 0.0360 mL | 0.1802 mL | 0.3603 mL | 0.9008 mL | |
| 80 mM | 0.0270 mL | 0.1351 mL | 0.2702 mL | 0.6756 mL | |
| 100 mM | 0.0216 mL | 0.1081 mL | 0.2162 mL | 0.5405 mL |
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