Tucidinostat 是一种有效的，可口服的 HDAC 第 I 类 HDAC1/2/3 和第 IIb 类 HDAC10 的抑制剂，IC50 值分别为 95，160，67 和 78 nM，对 HDAC8 和 HDAC11 的作用较弱 (IC50，733 nM，432 nM)，对 HDAC4/5/6/7/9 无作用。
CAS：1616493-44-7
分子式：C22H19FN4O2
分子量：390.41
纯度：98%
存储：Store at -20°C

Background:

Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9. HDAC3|67 nM (IC50)|HDAC10|78 nM (IC50)|HDAC1|95 nM (IC50)|HDAC2|160 nM (IC50)|HDAC11|432 nM (IC50)|HDAC8|733 nM (IC50)

Tucidinostat (Chidamide/CS055/HBI-8000) is a potent and orally bioavailable HDAC enzymes class I (HDAC1, 2, 3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9 (IC50s, >30 μM). Tucidinostat shows potent antitumor activity, and inhibits several human derived tumor cell lines, such as HL-60, U2OS, LNCaP with GI50s of 0.4 ± 0.1, 2.0 ± 0.6, and 4.0 ± 1.2 μM, respectively. In addition, Tucidinostat shows less toxic to normal cells from human fetal kidney (CCC-HEK) and liver (CCCHEL)[1].

Tucidinostat (12.5-50 mg/kg, p.o.) dose-dependently reduces tumor size and tumor weight in mice bearing HCT-8 colorectal carcinoma, A549 lung carcinoma, BEL-7402 liver carcinoma, and MCF-7 breast carcinoma, and with no obvious body loss[1].

[1]. Ning ZQ, et al. Chidamide (CS055/HBI-8000): a new histone deacetylase inhibitor of the benzamide class with antitumor activity and the ability to enhance immune cell-mediated tumor cell cytotoxicity. Cancer Chemother Pharmacol. 2012 Apr;69(4):901-9.