FB23-2 is a potent FTO inhibitor. FB23-2 demonstrated the potent inhibitory impact in AML models. FB23-2 directly binds to FTO and selectively inhibit FTO's m6A demethylase activity. Mimicking FTO depletion, FB23-2 dramatically suppresses proliferation and promotes the differentiation/apoptosis of human acute myeloid leukemia (AML) cell line cells and primary blast AML cells in vitro. Moreover, FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice. Collectively, our data suggest that FTO is a druggable target and that targeting FTO by small-molecule inhibitors holds potential to treat AML.
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名称 | FB23-2 |
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Iupac 化学名称 | 2-((2,6-dichloro-4-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-N-hydroxybenzamide |
同义词 | FB23-2; FB-23-2; FB 23-2; FB232; FB-232; FB 232; |
英文同义词 | FB23-2; FB-23-2; FB 23-2; FB232; FB-232; FB 232; |
分子式 | C18H15Cl2N3O3 |
分子量 | 392.236 |
Smile | O=C(NO)C1=CC=CC=C1NC2=C(Cl)C=C(C3=C(C)ON=C3C)C=C2Cl |
InChiKey | ILHNIWOZZKIBNW-UHFFFAOYSA-N |
InChi | InChI=1S/C18H15Cl2N3O3/c1-9-16(10(2)26-23-9)11-7-13(19)17(14(20)8-11)21-15-6-4-3-5-12(15)18(24)22-25/h3-8,21,25H,1-2H3,(H,22,24) |
Cas号 | 2243736-45-8 |
相关CAS号 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 固体粉末 |
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纯度 | 98% Min. |
存储 | 干燥,黑暗,短期(几天到几周)在0-4摄氏度,长期在-20摄氏度(几个月到几年) |
可溶性 | 可溶于DMSO |
处理方式 | |
运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关停留期间足够稳定几个星期。 |
海关编码 |
Targets | |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
1: Huang Y, Su R, Sheng Y, Dong L, Dong Z, Xu H, Ni T, Zhang ZS, Zhang T, Li C,
Han L, Zhu Z, Lian F, Wei J, Deng Q, Wang Y, Wunderlich M, Gao Z, Pan G, Zhong D,
Zhou H, Zhang N, Gan J, Jiang H, Mulloy JC, Qian Z, Chen J, Yang CG.
Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia.
Cancer Cell. 2019 Apr 15;35(4):677-691.e10. doi: 10.1016/j.ccell.2019.03.006.
PubMed PMID: 30991027.
2: Van Der Werf I, Jamieson C. The Yin and Yang of RNA Methylation: An Imbalance
of Erasers Enhances Sensitivity to FTO Demethylase Small-Molecule Targeting in
Leukemia Stem Cells. Cancer Cell. 2019 Apr 15;35(4):540-541. doi:
10.1016/j.ccell.2019.03.011. PubMed PMID: 30991023.