For research use only. Not for therapeutic Use.
Tefinostat（Cat No.:I009740）is a selective histone deacetylase (HDAC) inhibitor that primarily targets HDAC1, HDAC3, and HDAC9. It is designed as an anti-cancer agent, particularly for hematological malignancies such as chronic myelomonocytic leukemia (CMML). Tefinostat works by promoting histone acetylation, leading to the reactivation of tumor suppressor genes, inhibition of cell proliferation, and induction of apoptosis in cancer cells. Its selective targeting of HDACs aims to minimize off-target effects and toxicity. Tefinostat is also being explored for its potential in combination therapies for improved cancer treatment outcomes.
| Catalog Number | I009740 |
| CAS Number | 914382-60-8 |
| Synonyms | CHR-2845; CHR 2845; CHR2845; Tefinostat;cyclopentyl (S)-2-((4-(8-(hydroxyamino)-8-oxooctanamido)benzyl)amino)-2-phenylacetate |
| Molecular Formula | C28H37N3O5 |
| Purity | ≥95% |
| Target | Epigenetics |
| 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 |
| Reference | </br>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 Article</br>2: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 |
