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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-Tefinostat
Tefinostat

Chemical Structure : Tefinostat

CAS No.: 914382-60-8

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Tefinostat (CHR-2845, CHR2845)

货号: PC-21650Not For Human Use, Lab Use Only.

Tefinostat (CHR-2845) is a monocyte/macrophage targeted pan histone deacetylase (HDAC) inhibitor, which is cleaved into the active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Tefinostat (CHR-2845) is a monocyte/macrophage targeted pan histone deacetylase (HDAC) inhibitor, which is cleaved into the active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1).
Tefinostat show sselective high sensitivity against monocytoid leukaemias with EC50 of 57 nM to MV411 (M4, FLT3-ITD).
Tefinostat spares normal bone marrow progenitor cells.
hCE-1 expression levels dictate efficacy of Tefinostat in monocytic leukaemias.
Tefinostat is synergistic with cytarabine.

物理化学性质&存储条件

分子量 495.62
分子式 C28H37N3O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

cyclopentyl (2S)-2-[[4-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-2-phenylacetate

参考文献

1. Zabkiewicz J, et al. Oncotarget. 2016 Mar 29;7(13):16650-62.

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