Tefinostat

• CAT Number: I009740
• CAS Number: 914382-60-8
• Molecular Formula: C28H37N3O5
• Molecular Weight: 495.62
• Purity: ≥95%
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• IUPAC Name: cyclopentyl (2S)-2-[[4-[[8-(hydroxyamino)-8-oxooctanoyl]amino]phenyl]methylamino]-2-phenylacetate
• InChI: 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
• InChIKey: GLNWREBYRLDPQP-MHZLTWQESA-N
• SMILES: C1CCC(C1)OC(=O)C(C2=CC=CC=C2)NCC3=CC=C(C=C3)NC(=O)CCCCCCC(=O)NO

Tefinostat (Cat.No:I009740), also known as CHR-2845, is a monocyte/macrophage targeted histone deacetylase inhibitor (HDACi). Tefinostat produces monocyte-targeted HDACi activity and is well tolerated, without the DLTs, e.g. fatigue, diarrhoea, thrombocytopenia, commonly seen with non-targeted HDACi. The early signs of efficacy and absence of significant toxicity warrant further evaluation of tefinostat in larger studies.

Reference

1:The targeted histone deacetylase inhibitor tefinostat (CHR-2845) shows selective in vitro efficacy in monocytoid-lineage leukaemias. Zabkiewicz J, Gilmour M, Hills R, Vyas P, Bone E, Davidson A, Burnett A, Knapper S.Oncotarget. 2016 Mar 29;7(13):16650-62. doi: 10.18632/oncotarget.7692. PMID: 26934551 Free PMC Article2:A phase I first-in-human study with tefinostat – a monocyte/macrophage targeted histone deacetylase inhibitor – in patients with advanced haematological malignancies. Ossenkoppele GJ, Lowenberg B, Zachee P, Vey N, Breems D, Van de Loosdrecht AA, Davidson AH, Wells G, Needham L, Bawden L, Toal M, Hooftman L, Debnam PM.Br J Haematol. 2013 Jul;162(2):191-201. doi: 10.1111/bjh.12359. Epub 2013 May 7. PMID: 23647373