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Tefinostat

CAS No. : 914382-60-8

產(chǎn)品活性：Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias.

研究領(lǐng)域：Cell Cycle/DNA Damage  |  Epigenetics  |  Apoptosis

作用靶點：HDAC  |  Apoptosis

In Vitro: Tefinostat (CHR-2845) (1-4 nM) has efficacy in AML cell lines HL60 (M2 FAB type), MV411 (M4, FLT3-ITD), OCIAML3 (M4 NPM1mut) and THP1 (M5) with EC₅₀ values of 2.3 μM, 57 nM, 110 nM and 560 nM, respectively.
Tefinostat (0, 0.5, 1 and 5μM; 24, 48 h) has dose-dependent induction of apoptosis and significant growth inhibitory effects.

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