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 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 EC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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. Form:Solid IC50& Target:HDAC
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
Tefinostat
CAS number：914382-60-8 molecular formula：C28H37N3O5
overview
compound introduction
Specs
| Chinese alias | 特非司他 | ||
| English alias | HY-106409 | SCHEMBL1491466 | Tefinostat [INN] | UNII-ZAU91150SB | cyclopentyl (S)-2-((4-(8-(hydroxyamino)-8-oxooctanamido)benzyl)amino)-2-phenylacetate | Benzeneacetic acid, alpha-(((4-((8-(hydroxyamino)-1,8-dioxooctyl)amino)phenyl)methyl)amino)-, cyclope | ||
| CAS number | 914382-60-8 | molecular formula | C28H37N3O5 |
| molecular weight | 495.61 g/mol | Exact mass | ≥98% |
| PSA | 117.000 Ų | logp | 3.800 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
