An inhibitor of HDACs and a prodrug form of CHR-2847
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Tefinostat

Item No. 43665

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
αS-[[[4-[[8-(hydroxyamino)-1,8-dioxooctyl]amino]phenyl]methyl]amino]-benzeneacetic acid, cyclopentyl ester
CAS Number
914382-60-8
Molecular Formula
C28H37N3O5
Formula Weight
495.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(OC1CCCC1)[C@H](C2=CC=CC=C2)NCC3=CC=C(C=C3)NC(CCCCCCC(NO)=O)=O
InChi Code
InChI=1S/C28H37N3O5/c32-25(14-6-1-2-7-15-26(33)31-35)30-23-18-16-21(17-19-23)20-29-27(22-10-4-3-5-11-22)28(34)36-24-12-8-9-13-24/h3-5,10-11,16-19,24,27,29,35H,1-2,6-9,12-15,20H2,(H,30,32)(H,31,33)/t27-/m0/s1
InChi Key
GLNWREBYRLDPQP-MHZLTWQESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $87

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    5 mg

    $326

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    10 mg

    $479

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    25 mg

    $761

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    Cayman Chemical
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    Product Description

    Tefinostat is a monocyte-selective pan-inhibitor of histone deacetylases (HDACs) and a prodrug form of CHR-2847.1 It is converted to CHR-2847 by carboxylesterase 1 (CES1), which is selectively expressed in monocyte lineage cells, as well as some hepatocytes. Tefinostat increases intracellular protein acetylation in CD14+ primary human acute myeloid leukemia (AML) cells and gamma histone H2AX (γH2AX) levels in primary chronic myelomonocytic leukemia (CMML) cells in a concentration-dependent manner. It selectively inhibits the growth of primary AML cells over normal bone marrow cells when used at a concentration of 500 nM. Tefinostat (2 µM) induces β-oxidation of the very long-chain fatty acid hexacosanoic acid (Item No. 13354) in primary human macrophages.2 It also inhibits the migration of isolated human peripheral blood mononuclear cells (PBMCs) toward supernatant isolated from LPS-stimulated primary human macrophages.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zabkiewicz, J., Gilmour, M., Hills, R., et al. The targeted histone deacetylase inhibitor tefinostat (CHR-2845) shows selective in vitro efficacy in monocytoid-lineage leukaemias. Oncotarget 7(13), 16650-16662 (2016).

    2. Villoria-González, A., Zierfuss, B., Parzer, P., et al. Efficacy of HDAC inhibitors in driving peroxisomal β-oxidation and immune responses in human macrophages: Implications for neuroinflammatory disorders. Biomolecules 13(12), 1696 (2023).