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10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
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.
IC50& Target:HDAC
| Isomeric SMILES | C1CCC(C1)OC(=O)[C@H](C2=CC=CC=C2)NCC3=CC=C(C=C3)NC(=O)CCCCCCC(=O)NO |
|---|---|
| Alternate CAS | 914382-60-8 |
| PubChem CID | 15940949 |
| MeSH Entry Terms | CHR 2845;tefinostat |
| Molecular Weight | 495.61 |
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