Tucidinostat (Chidamide) (C09-1074-471)

InformationTucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor ofHDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.TargetsHDAC3 (Cell-free); HDAC10 (Cell-free); HDAC1 (Cell-free); HDAC2 (Cell-free) 67 nM ;78 nM; 95 nM; 160 nMIn vitroChidamide inhibits class I HDACs 1-3, as well as class IIb HDAC10, at low nanomolar concentrations. Chidamide significantly induces histone H3 acetylation in both HeLa human cervical adenocarcinoma cells and human PBMC. Cell growth inhibition studies performed with 18 human-derived tumor cell lines demonstrate that chidamide and MS-275 similarly inhibit the in vitro growth of most, but not all, tumor cells in the low micromolar concentration range. However, chidamide, and to a lesser extent MS-275, is significantly less toxic to normal cells from human fetal kidney (CCC-HEK) and liver (CCC-HEL), indicating a differential cytotoxic response of normal cells versus cancerous cells to chidamide.In vivoIn HCT-8 colorectal carcinoma mice xenografts, Chidamide shows in vivo antitumor activity. Chidamide in the dose range of 12.5-50 mg/kg dose-dependently reduces tumor size and tumor weight, and the dose of 50 mg/kg produces similar or greater efficacy compared with the control drugs 5-fluorouracil(5-FU, 20 mg/kg) and MS-275 (25 mg/kg, which was reported as the maximum tolerated dose in xenograft models). However, chidamide is well-tolerated at the above doses in the tumor-bearing animals, whereas the control drugs cause significant weight loss.Cell Research(from reference)Cell lines：PBMC effector cells Concentrations：0-400 nM Incubation Time：0-400 nM. Specifications and Purity: 98%. Molecular Formula: C22H19FN4O2. Molecular Weight: 390.41. PubChem CID: 12136798. Isomeric SMILES: C1=CC(=CN=C1)/C=C/C(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N. Related Document: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/T414062-SCI_fe9da2aba0ee5a2be49b7c04495a1a2c.pdf.