Art. -Nr.: HY-19540

GSK864

Name: GSK864
Brand: MedChemExpress
SKU: HY-19540
Price: 190.00 USD
Availability: InStock
Rating: 5 (8 reviews)

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

GSK864, a chemical probe, is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC₅₀ values of 8.8, 15.2 and 16.6 nM.

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Reinheit : 99.91%
CAS. Nr.: 1816331-66-4
Formel: C₃₀H₃₁FN₆O₄
Molecular Weight:558.60

Speicherung:

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

GSK864 Chemical Structure

CAS. Nr.: 1816331-66-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (1)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GSK864, a chemical probe, is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC₅₀ values of 8.8, 15.2 and 16.6 nM.

IC₅₀ & Target

IDH1

Alle Isocitrate Dehydrogenase (IDH) Isoform-spezifische Produkte anzeigen :

IDH1
IDH2

In Vitro

GSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells with an EC₅₀ of 320 nM by LCMS/MS analysis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

Following intraperitoneal (IP) administration in CD-1 mice, significant concentrations of GSK864 are maintained in peripheral blood samples of mice for up to 24 hours. Analysis of BM cells for expression of markers of early differentiation reveals slightly increased numbers of huCD45⁺ CD38⁺ cells in R132C or R132H IDH1 mutant engrafted mice treated with GSK864^[1].

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

Chemical Information

CAS. Nr. 1816331-66-4
Appearance Solid
Molecular Weight 558.60
Formel C₃₀H₃₁FN₆O₄
Color Light brown to brown
SMILES

FC(C=C1)=CC=C1CN2N=C(C(NC3=CC(C)=C(OC)C(C)=C3)=O)C4=C2[C@](C(N)=O)(C)CN(C(C5=CC=CN5)=O)C4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (8)

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Journal Impact Factor

Nature

αKG-mediated carnitine synthesis drives DNA repair via histone acetylation. [Abstract]

2026 Jul;655(8123):790-800. PMID: 42203879
Gut

HNF4α pathway mapping identifies wild-type IDH1 as a targetable metabolic node in gastric cancer. [Abstract]

2020 Feb;69(2):231-242. PMID: 31068366
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
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

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
Nat Chem Biol

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

2026 Jan 13. PMID: 41530531
ACS Med Chem Lett

Synthesis and Evaluation of a 18F-Labeled Triazinediamine Analogue for Imaging Mutant IDH1 Expression in Gliomas by PET. [Abstract]

2018 May 1;9(7):606-611. PMID: 30034587
bioRxiv

αKG-mediated carnitine synthesis promotes homologous recombination via histone acetylation. [Abstract]

2024 Feb 11:2024.02.06.578742. PMID: 38370789

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (179.02 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

1.7902 mL

8.9509 mL

17.9019 mL

5 mM

0.3580 mL

1.7902 mL

3.5804 mL

10 mM

0.1790 mL

0.8951 mL

1.7902 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.48 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 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 (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Protokoll

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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)
Handling Instructions (2659 KB)

Verweise

[1]. Okoye-Okafor UC, et al. New IDH1 mutant inhibitors for treatment of acute myeloid leukemia. Nat Chem Biol. 2015 Nov;11(11):878-86. [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, 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	1 mM	1.7902 mL	8.9509 mL	17.9019 mL	44.7547 mL
	5 mM	0.3580 mL	1.7902 mL	3.5804 mL	8.9509 mL
	10 mM	0.1790 mL	0.8951 mL	1.7902 mL	4.4755 mL
	15 mM	0.1193 mL	0.5967 mL	1.1935 mL	2.9836 mL
	20 mM	0.0895 mL	0.4475 mL	0.8951 mL	2.2377 mL
	25 mM	0.0716 mL	0.3580 mL	0.7161 mL	1.7902 mL
	30 mM	0.0597 mL	0.2984 mL	0.5967 mL	1.4918 mL
	40 mM	0.0448 mL	0.2238 mL	0.4475 mL	1.1189 mL
	50 mM	0.0358 mL	0.1790 mL	0.3580 mL	0.8951 mL
	60 mM	0.0298 mL	0.1492 mL	0.2984 mL	0.7459 mL
	80 mM	0.0224 mL	0.1119 mL	0.2238 mL	0.5594 mL
	100 mM	0.0179 mL	0.0895 mL	0.1790 mL	0.4475 mL

Bioz

Keywords

GSK864

8 Cited Publications

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GSK864

Publications Citing Use of MedChemExpress (MCE) GSK864

Alle Isocitrate Dehydrogenase (IDH) Isoform-spezifische Produkte anzeigen