Tucidinostat

• CAT Number: I009908
• CAS Number: 1616493-44-7
• PubChem Substance ID: 12136798
• Molecular Formula: C22H19FN4O2
• Molecular Weight: 390.41
• Purity: ≥95%
• Target: Histone Deacetylase Inhibitor
• Solubility: Soluble in DMSO
• Storage: Store at -20°C
• IUPAC Name: N-(2-amino-4-fluorophenyl)-4-[[[(E)-3-pyridin-3-ylprop-2-enoyl]amino]methyl]benzamide
• InChI: InChI=1S/C22H19FN4O2/c23-18-8-9-20(19(24)12-18)27-22(29)17-6-3-16(4-7-17)14-26-21(28)10-5-15-2-1-11-25-13-15/h1-13H,14,24H2,(H,26,28)(H,27,29)/b10-5+
• InChIKey: SZMJVTADHFNAIS-BJMVGYQFSA-N
• SMILES: C1=CC(=CN=C1)C=CC(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N

Tucidinostat, also known as Chidamide, HBI-8000, and CS-055, is a potent inhibitor of HDAC1, 2, 3, and 10, with IC50 values of 95, 160, 67, and 78 nM, respectively. This low molar concentration inhibitor of histone deacetylases (HDACs) has shown promising results in clinical trials for the treatment of various cancers, including lymphoma and leukemia.

Reference

1: Gao S, Li X, Zang J, Xu W, Zhang Y. Preclinical and clinical studies of chidamide (CS055/HBI-8000), an orally available subtype-selective HDAC inhibitor for cancer therapy. Anticancer Agents Med Chem. 2016 Sep 1. [Epub ahead of print] PubMed PMID: 27592546.2:Hasegawa H, Bissonnette RP, Gillings M, Sasaki D, Taniguchi H, Kitanosono H, Tsuruda K, Kosai K, Uno N, Morinaga Y, Imaizumi Y, Miyazaki Y, Yanagihara K. Induction of apoptosis by HBI-8000 in adult T-cell leukemia/lymphoma is associated with activation of Bim and NLRP3. Cancer Sci. 2016 Aug;107(8):1124-33. doi: 10.1111/cas.12971. Epub 2016 Jun 22. PubMed PMID: 27193821; PubMed Central PMCID: PMC4982578.3:Dong M, Ning ZQ, Xing PY, Xu JL, Cao HX, Dou GF, Meng ZY, Shi YK, Lu XP, Feng FY. Phase I study of chidamide (CS055/HBI-8000), a new histone deacetylase inhibitor, in patients with advanced solid tumors and lymphomas. Cancer Chemother Pharmacol. 2012 Jun;69(6):1413-22. doi: 10.1007/s00280-012-1847-5. Epub 2012 Feb 24. PubMed PMID: 22362161.