Chemical Structure : Tefinostat
CAS No.: 914382-60-8
Catalog No.: 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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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.
M.Wt | 495.62 | |
Formula | C28H37N3O5 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
cyclopentyl (2S)-2-[[4-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-2-phenylacetate |
1. Zabkiewicz J, et al. Oncotarget. 2016 Mar 29;7(13):16650-62.
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