AGI-6780

製品コードS7241 バッチS724102

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21 H18 F3 N3 O3 S2
分子量 481.51 CAS No. 1432660-47-3
Solubility (25°C)* 体外 DMSO 96 mg/mL (199.37 mM)
Ethanol 96 mg/mL (199.37 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明 AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.
in vitro AGI-6780 potently reduce (R)-2-hydroxyglutarate (2HG) levels in cell lines ectopically overexpressing IDH2/R140Q with EC50 of 20 nM, with excellent selectivity against other dehydrogenases. AGI-6780 reverses the IDH2/R140Q-induced differentiation block in TF-1 cells, and induces blast differentiation in primary human IDH2/R140Q AML patient samples. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Enzymatic assay of IDH inhibitors
Compound is prepared as 10 mM stock in DMSO and diluted to 50X final concentration in DMSO, for a 50 μL reaction mixture. IDH enzyme activity converting alpha-ketoglutarate to 2-hydroxyglutarate is measured using a NADPH depletion assay. In the assay the remaining cofactor is measured at the end of the reaction with the addition of a catalytic excess of diaphorase and resazurin, to generate a fluorescent signal in proportion to the amount of NADPH remaining. IDH enzyme activity in the direction of isocitrate to alpha-ketoglutarate conversion is measured by direct coupling of the NADPH production to conversion of resazurin to resorufin by diaphorase. In both cases, resorufin is measured fluorometrically at Ex544 Em 590. For assay of the IDH2/R140Q homodimer and the IDH2-R140Q/WT heterodimer, protein is diluted to 0.31 μg/ml in 40 μl Assay Buffer (150 mM NaCl, 50 mM 3 potassium phosphate pH 7.5, 10 mM MgCl2, 10% glycerol, 0.05% BSA, 2 mM β-mercapoethanol) containing 5 μM NADPH. 1 μl of 50X compound dilution is added and the mixture and incubated for 16 hours at 25°C. The enzymatic reaction is started with the addition of 10 μl of Assay Buffer containing 8 mM alpha-ketoglutarate and incubated at 25°C for 60 minutes. The reaction is stopped with the addition of Detection Buffer (1X Assay Buffer containing 36 μg/ml diaphorase and 18 μM resazurin), incubated for five minutes at room temperature, and read on a SpectraMax 384 platereader.

カスタマーフィードバック

Data from [Data independently produced by , , Blood, 2018, doi: 10.1182/blood-2018-05-850826]

Data from [Data independently produced by , , Theranostics, 2018, 8(15):4050-4061]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Targeting PRMT1 prevents acute and chronic graft-versus-host disease [ Mol Ther, 2023, 10.1016/j.ymthe.2023.09.011] PubMed: 37735873
IDH2 stabilizes HIF-1α-induced metabolic reprogramming and promotes chemoresistance in urothelial cancer [ EMBO J, 2023, e110620.] PubMed: 36637036
Aberrant metabolite trafficking and fuel sensitivity in human pluripotent stem cell-derived islets [ Cell Rep, 2023, 42(8):112970] PubMed: 37556323
Targeting Mitochondrial IDH2 Enhances Antitumor Activity of Cisplatin in Lung Cancer via ROS-Mediated Mechanism [ Biomedicines, 2023, 11(2)475] PubMed: 36831011
Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] PubMed: 35868306
Reductive TCA cycle catalyzed by wild-type IDH2 promotes acute myeloid leukemia and is a metabolic vulnerability for potential targeted therapy [ J Hematol Oncol, 2022, 15(1):30] PubMed: 35313945
Comprehensive drug response profiling and pan-omic analysis identified therapeutic candidates and prognostic biomarkers for Asian cholangiocarcinoma [ iScience, 2022, 25(10):105182] PubMed: 36248745
Mitofusin2 Promotes β Cell Maturation from Mouse Embryonic Stem Cells via Sirt3/Idh2 Activation [ Stem Cells Int, 2022, 2022:1172795] PubMed: 35386849
Wild-type IDH2 protects nuclear DNA from oxidative damage and is a potential therapeutic target in colorectal cancer [ Oncogene, 2021, 10.1038/s41388-021-01968-2] PubMed: 34349242
Biomimetic mesoporous vectors enabling the efficient inhibition of wild-type isocitrate dehydrogenase in multiple myeloma cells [ Elsevier, 2021, 10.1016/j.micromeso.2021.111320] PubMed: N/A

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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