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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
中文名称
Tefinostat
英文名称
Tefinostat
中文别名
特非司他
英文别名
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号
914382-60-8
分子式
C28H37N3O5
分子量
495.61 g/mol
精确质量
≥98%
PSA
117.000 Ų
Logp
3.800
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Tefinostat 1ml

品牌:阿拉丁
货号:T655020-1ml
级别: 10mM in DMSO
货期:30天
已售 535 件
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1ml

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