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AGI-6780

AGI6780 能够选择性抑制肿瘤相关突变体IDH2R140Q，IC50=23±1.7 nM。它对IDH2WT 的作用效果微弱，IC50=190±8.1 nM。

CAS号

1432660-47-3

分子式

C21H18F3N3O3S2

主要靶点

Isocitrate Dehydrogenase (IDH)|Dehydrogenase

仅限科研使用

Cat No : CM04694

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Synonyms

验证数据展示

  • CAS No.: 1432660-47-3

    AGI-6780
    CAS#: 1432660-47-3

产品信息

AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant.

CAS号 1432660-47-3
分子式 C21H18F3N3O3S2
主要靶点 Isocitrate Dehydrogenase (IDH)|Dehydrogenase
主要通路 代谢
分子量 481.51
纯度 98.15%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

IDH2 R140Q mutant:23 nM

体内活性

AGI-6780逆转TF-1细胞中IDH2/ R140Q诱导的分化阻滞,并诱导原发性人类IDH2/R140Q AML患者样品中的急剧分化。AGI-6780有效降低异位过表达IDH2/R140Q的细胞系中的（R）-2-羟基戊二酸（2 hG）水平,EC 50为20 nM,与其他脱氢酶相比,具有优异的选择性。

溶解度

DMSO:89 mg/mL (184.8 mM),Ethanol:89 mg/mL (184.8 mM),H2O:<1 mg/mL

细胞实验

AGI-6780 is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. Cells are sorted from fresh or frozen bone marrow aspirates and blood samples after labelling with PE-CD34, APC-CD38, PE-CD14, FITC-CD3 (clone HIT3a) and PECy7-CD19 (clone SJ25C1) antibodies using a MoFlow cell sorter. Unfractionated nucleated blood or bone marrow cells are plated in Methocult H4434 methylcellulose medium at 104 cells/dish, in duplicate dishes per condition. AGI-6780 (5 mM) is directly added to the medium. Dishes are incubated in a humidified incubator at 37°C and colonies containing at least 30 cells are counted after 13 days[1].

参考文献

1.Wang F, et al. Science. 2013, 340(6132), 622-666.
2.Chen J, Yang J, Wei Q, et al. Cell Communication and Signaling. 2020, 18(1): 1-12.
3.Chen J, Yang J, Wei Q, et al. Identification of a selective inhibitor of IDH2/R140Q enzyme that induces cellular differentiation in leukemia cells[J]. Cell Communication and Signaling. 2020, 18: 1-12.
4.Chen J, Yang J, Wei Q, et al. Identification of a selective inhibitor of IDH2/R140Q enzyme that induces cellular differentiation in leukemia cells[J]. Cell Communication and Signaling . 2020, 18: 1-12.

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