Tefinostat

Research use only, not for human use.

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

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.

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.Cell Viability Assay Cell Line:AML cell lines Concentration:1-4 nM Incubation Time:Result:Had significant growth inhibitory effects.Apoptosis AnalysisCell Line:myelo-monocytic cell lines and HL60 cells Concentration:0, 0.5, 1 and 5μM Incubation Time:24, 48 h Result:Showed strong apoptotic induction in myelo-monocytic cell lines THP1, MV411 (FLT3-ITD) and OCIAML3 within 24 hours and only reached in nonmonocytic HL60 cells at much higher concentrations.

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Cell Cycle/DNA Damage

HDAC

HDAC

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914382-60-8

495.61

C28H37N3O5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (201.77 mM; Ultrasonic )

ONC(=O)CCCCCCC(=O)Nc1ccc(CN[C@H](C(=O)OC2CCCC2)c2ccccc2)cc1

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(-20℃)

With Ice Pack

≥ 2 years