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别名:
2,3-Dihydro-N-hydroxy-1,1-dimethyl-2-[5-(trifluoromethyl)-2-pyrazinyl]-1H-isoindole-4-carboxamide, FT 895, FT-895, HDTK 070, HDTK-070, HDTK070, N-Hydroxy-1,1-dimethyl-2-(5-(trifluoromethyl)pyrazin-2-yl)isoindoline-4-carboxamide
经验公式（希尔记法）:
C16H15F3N4O2
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生化/生理作用
FT895 is a potent and highly selective HDAC11 inhibitor (IC50 = 3 nM/HDAC11, 5.6 μM/HDAC8, >10 μM/HDAC1-7, HDAC9 & HDAC10) with a deacetylase active site Zn2+-targeting hydroxamate. FT895 exhibits antiproliferation potency against myeloproliferative neoplasm (MPN) cultures (IC50 = 3.00 μM/JAK2(V617F) Ba/F3, 4.94 μM/HEL92.1.7, 6.49 μM/MPL(W515L) Ba/F3) and reduces stem-like properties of CSCs (42/62/85/100% inhibtion of H1650 Sphere formation at 0.5/1/2/5 μM).
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
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Matthew W Martin et al.
Bioorganic & medicinal chemistry letters, 28(12), 2143-2147 (2018-05-20)
N-Hydroxy-2-arylisoindoline-4-carboxamides are potent and selective inhibitors of HDAC11. The discovery, synthesis, and structure activity relationships of this novel series of inhibitors are reported. An advanced analog (FT895) displays promising cellular activity and pharmacokinetic properties that make it a useful tool
Se In Son et al.
ACS chemical biology, 14(7), 1393-1397 (2019-07-03)
Mammalian histone deacetylases (HDACs) are a class of enzymes that play important roles in biological pathways. Existing HDAC inhibitors target multiple HDACs without much selectivity. Inhibitors that target one particular HDAC will be useful for investigating the biological functions of
Namrata Bora-Singhal et al.
Scientific reports, 10(1), 4722-4722 (2020-03-15)
Non-small cell lung cancer (NSCLC) is known to have poor patient outcomes due to development of resistance to chemotherapy agents and the EGFR inhibitors, which results in recurrence of highly aggressive lung tumors. Even with recent success in immunotherapy using
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