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Tefinostat

Chemical Structure : Tefinostat

CAS No.: 914382-60-8

Tefinostat (CHR-2845, CHR2845)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 495.62
Formula C28H37N3O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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

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