Tucidinostat-Chidamide-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETucidinostatCat. No.: HY-109015CAS No.: 1616493-44-7Synonyms: Chidamide; HBI-8000; CS 055分式: CHFNO分量: 390.41作靶點: HDAC作通路: Cell Cycle/DNA Damage; Epigenetics儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解

2、性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (128.07 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.5614 mL 12.8070 mL 25.6141 mL5 mM 0.5123 mL 2.5614 mL 5.1228 mL10 mM 0.2561 mL 1.2807 mL 2.5614 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢?/p>

3、先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.40 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.40 mM); Clear solution1/2

4、Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.40 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Tucidinostat種有效的，可服的 HDAC 第 I 類 HDAC1/2/3 和第 IIb 類 HDAC10 的抑制劑，IC50 值分別為 95，160，67 和 78 nM，對 HDAC8 和 HDAC11 的作較弱 (IC50，733 nM，432 nM)，對 HDAC4/5/6/7/9作

5、。IC50 & Target HDAC3 HDAC10 HDAC1 HDAC267 nM (IC50) 78 nM (IC50) 95 nM (IC50) 160 nM (IC50)HDAC11 HDAC8432 nM (IC50) 733 nM (IC50)體外研究 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

6、, 67 and 78 nM, less active on HDAC8and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9 (IC50s, 30 M). Tucidinostat shows potent antitumor activity, and inhibits several human derived tumor cell lines, such asHL-60, U2OS, LNCaP with GI50s of 0.4 0.1, 2.0 0.6, and 4

7、.0 1.2 M, respectively. In addition,Tucidinostat shows less toxic to normal cells from human fetal kidney (CCC-HEK) and liver (CCCHEL) 1.體內(nèi)研究 Tucidinostat (12.5-50 mg/kg, p.o.) dose-dependently reduces tumor size and tumor weight in mice bearingHCT-8 colorectal carcinoma, A549 lung carcinoma, BEL-74

8、02 liver carcinoma, and MCF-7 breast carcinoma,and with no obvious body loss 1.REFERENCES1. Ning ZQ, et al. Chidamide (CS055/HBI-8000): a new histone deacetylase inhibitor of the benzamide class with antitumor activity and theability to enhance immune cell-mediated tumor cell cytotoxicity. Cancer Chemother Pharmacol. 2012 Apr;69(4):901-9.McePdfHeightCaution: Product has not been fully validated for medical applicatio