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Tefinostat
CAS No. 914382-60-8
Tefinostat( —— )
Catalog No. M33515 CAS No. 914382-60-8
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).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 245 | In Stock |
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| 5MG | 227 | In Stock |
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| 10MG | 337 | In Stock |
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| 25MG | 510 | In Stock |
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| 50MG | 662 | In Stock |
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| 100MG | 1042 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameTefinostat
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NoteResearch use only, not for human use.
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Brief DescriptionTefinostat (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).
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DescriptionTefinostat (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.
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In VitroTefinostat (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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In Vivo——
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Synonyms——
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PathwayCell Cycle/DNA Damage
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TargetHDAC
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RecptorHDAC
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Research Area——
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Indication——
Chemical Information
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CAS Number914382-60-8
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Formula Weight495.61
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Molecular FormulaC28H37N3O5
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (201.77 mM; Ultrasonic )
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SMILESONC(=O)CCCCCCC(=O)Nc1ccc(CN[C@H](C(=O)OC2CCCC2)c2ccccc2)cc1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Zabkiewicz J, et al. The targeted histone deacetylase inhibitor tefinostat (CHR-2845) shows selective in vitro efficacy in monocytoid-lineage leukaemias. Oncotarget. 2016 Mar 29;7(13):16650-62.?
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