Vorasidenib
Based on 7 publication(s) in Google Scholar
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. Vorasidenib can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.76%
- No. CAS: 1644545-52-7
- Fòrmula: C14H13ClF6N6
- Peso molecular:414.74
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Vorasidenib
More- Science. 2024 Jul 12;385(6705):eadl6173. [Abstract]
- Imeta. 2026 Feb 12.
- Theranostics. 2020 Jul 9;10(19):8757-8770. [Abstract]
- J Med Chem. 2023 Apr 13;66(7):5279-5288. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Metabolites. 2021 Feb 13;11(2):109. [Abstract]
- bioRxiv. 2026 Feb 2:2026.01.30.702627. [Abstract]
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Imaging
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Actividad biológica
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IDH1 |
IDH2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | IC50 |
<50 nM
Compound: 98; AG-881
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Antiproliferative activity against human HT1080 cells after 72 hrs by celltiterglo reagent based assay
Antiproliferative activity against human HT1080 cells after 72 hrs by celltiterglo reagent based assay
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[PMID: 29847930] |
| U-87MG ATCC | IC50 |
<50 nM
Compound: 98; AG-881
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Antiproliferative activity against human U87MG cells expressing pLVX-IDH2 R140Q mutant after 72 hrs by celltiterglo reagent based assay
Antiproliferative activity against human U87MG cells expressing pLVX-IDH2 R140Q mutant after 72 hrs by celltiterglo reagent based assay
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[PMID: 29847930] |
Vorasidenib has strong antiproliferative activity against human glioblastoma U-87 MG pLVX-IDH2 R140Q-neo, fibrosarcoma HT-1080 and neurosphere TS603 cells, all with IC50s of less than 50 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1644545-52-7
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Appearance Solid
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Peso molecular 414.74
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Fòrmula C14H13ClF6N6
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Color White to off-white
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SMILES
C[C@@H](NC1=NC(C2=NC(Cl)=CC=C2)=NC(N[C@H](C)C(F)(F)F)=N1)C(F)(F)F
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Synonyms
AG-881
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (7)
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Journal Impact Factor
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Most Recent
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Science
2024 Jul 12;385(6705):eadl6173. PMID: 38991060 -
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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 Med Chem
Differentiating Inhibition Selectivity and Binding Affinity of Isocitrate Dehydrogenase 1 Variant Inhibitors. [Abstract]2023 Apr 13;66(7):5279-5288. PMID: 36952395 -
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 -
Metabolites
2021 Feb 13;11(2):109. PMID: 33668509
Vorasidenib purchased from MedChemExpress. Usage Cited in: Metabolites. 2021 Feb 13;11(2):109. [Abstract]
AG-881 (50 mg/kg; p.o.). Temporal evolution of average U87IDHmut tumor volume as a percentage of D0.
Vorasidenib purchased from MedChemExpress. Usage Cited in: Metabolites. 2021 Feb 13;11(2):109. [Abstract]
AG-881 (50 mg/kg; p.o.). Quantification of 2-HG, Glu and GLX concentrations acquired from the voxel placed in control, AG-881- and BAY-1436032-treated tumors at D5 ± 1.
Vorasidenib purchased from MedChemExpress. Usage Cited in: Metabolites. 2021 Feb 13;11(2):109. [Abstract]
AG-881 (50 mg/kg; p.o.). Representative axial T2-weighted images of control (top line, blue), AG-881 (middle line purple) and BAY-1436032 (bottom line orange)-treated BT257 tumor-bearing mice at D0, D7 ± 2 and D15 ± 1.
Vorasidenib purchased from MedChemExpress. Usage Cited in: Metabolites. 2021 Feb 13;11(2):109. [Abstract]
AG-881 (50 mg/kg; p.o.). Kaplan-Meier survival plot of BT257 tumor-bearing mice treated with either AG-881 or BAY-1436032 when compared to controls.
Vorasidenib purchased from MedChemExpress. Usage Cited in: Metabolites. 2021 Feb 13;11(2):109. [Abstract]
AG-881 (50 mg/kg; p.o.). Quantification of 2-HG, Glu and GLX metabolites in control, AG-881- and BAY-1436032-treated tumors at D7 ± 2 and D15 ± 1 in the BT257.
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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
Solvente y solubilidad
DMSO : 100 mg/mL (241.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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 (5.02 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 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 (5.02 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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 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 | 2.4111 mL | 12.0557 mL | 24.1115 mL | 60.2787 mL |
| 5 mM | 0.4822 mL | 2.4111 mL | 4.8223 mL | 12.0557 mL | |
| 10 mM | 0.2411 mL | 1.2056 mL | 2.4111 mL | 6.0279 mL | |
| 15 mM | 0.1607 mL | 0.8037 mL | 1.6074 mL | 4.0186 mL | |
| 20 mM | 0.1206 mL | 0.6028 mL | 1.2056 mL | 3.0139 mL | |
| 25 mM | 0.0964 mL | 0.4822 mL | 0.9645 mL | 2.4111 mL | |
| 30 mM | 0.0804 mL | 0.4019 mL | 0.8037 mL | 2.0093 mL | |
| 40 mM | 0.0603 mL | 0.3014 mL | 0.6028 mL | 1.5070 mL | |
| 50 mM | 0.0482 mL | 0.2411 mL | 0.4822 mL | 1.2056 mL | |
| 60 mM | 0.0402 mL | 0.2009 mL | 0.4019 mL | 1.0046 mL | |
| 80 mM | 0.0301 mL | 0.1507 mL | 0.3014 mL | 0.7535 mL | |
| 100 mM | 0.0241 mL | 0.1206 mL | 0.2411 mL | 0.6028 mL |
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