Vorasidenib (Synonyms: AG-881)

Name: Vorasidenib
Brand: MedChemExpress
SKU: HY-104042
Rating: 5.0 (7 reviews)

Cat. No.: HY-104042 Purity: 99.76%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

For research use only. We do not sell to patients.

CAS No. : 1644545-52-7

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	Get quote
10 g	Get quote

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Vorasidenib:

Vorasidenib (Standard) Get quote

7 Publications Citing Use of MCE Vorasidenib

•bioRxiv. 2026 Feb 2:2026.01.30.702627.

In Vivo Efficacy Study

In Vivo Imaging

: 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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View All Isoforms

IDH1 IDH2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IDH1

IDH2

Cellular Effect

Cell Line	Type	Value	Description	References
HT-1080	IC₅₀	< 50 nM Compound: 98; AG-881	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	[PMID: 29847930]
U-87MG ATCC	IC₅₀	< 50 nM Compound: 98; AG-881	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	[PMID: 29847930]

In Vitro

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.

Clinical Trial

Molecular Weight

414.74

Formula

C₁₄H₁₃ClF₆N₆

CAS No.

1644545-52-7

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4111 mL	12.0557 mL	24.1115 mL
5 mM	0.4822 mL	2.4111 mL	4.8223 mL
10 mM	0.2411 mL	1.2056 mL	2.4111 mL

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (6.03 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.4 mg/mL (5.79 mM); Suspended solution; Need ultrasonic
Protocol 3

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.
Protocol 4

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.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.08 mg/mL (5.02 mM); Clear solution; Need warming

This protocol yields a clear solution of 2.08 mg/mL. 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.76%

Select Batch:

Data Sheet (274 KB) SDS (396 KB)

COA (249 KB) HNMR (193 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Fujii T, et al. Targeting isocitrate dehydrogenase (IDH) in cancer. Discov Med. 2016 May;21(117):373-80. [Content Brief]

[2]. Ma T, et al. Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective. J Med Chem. 2018 Oct 25;61(20):8981-9003. [Content Brief]

Complete Stock Solution Preparation Table

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

Vorasidenib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vorasidenib1644545-52-7AG-881AG881AG 881Isocitrate Dehydrogenase (IDH)Inhibitorinhibitorinhibit

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Vorasidenib (Synonyms: AG-881)

Customer Review

Other Forms of Vorasidenib:

Vorasidenib Related Antibodies

7 Publications Citing Use of MCE Vorasidenib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Isocitrate Dehydrogenase (IDH) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Vorasidenib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Vorasidenib Related Classifications

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Customer Review

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