S80927 |
Chidamide |
| 源叶(MedMol) | 96% |
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- 产品描述： HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable inhibitor of HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10).
- 靶点： HDAC
- 体内研究：
Inhibition of tumor growth by Chidamide (CS055) treatment is observed in a dose-dependent manner, demonstrating the anti-tumor activity of Chidamide. Control tumors grow to an average volume of 14.51 cm3 after 20 days, and Chidamide-treated tumors grow to 11.68, 11.05 and 8.45 cm3, corresponding to 19.54%, 23.83% and 41.80% growth inhibition respectively. The average tumor mass in animals treated with vehicle is 9.4±2.7 g and is 8.4±2.4 g for animals treated with low-dose Chidamide. In animals treated with a moderate dose of Chidamide, tumor mass is 7.6±1.6 g and those receiving high-dose Chidamide has a tumor mass of 5.4±1.5 g (P<0.01). Additionally, Chidamide treatment prolongs the survival of nude mice bearing HL60 xenografts. Moreover, the level of lipid peroxidation product (MDA), which is a presumptive measure of ROS-mediated injury, is increased in tumor tissue accompanied by treatment of Chidamide, suggesting that Chidamide-induced ROS generation might play a role
- 细胞实验： Chidamide (CS055) is dissolved in DMSO and stored, and then diluted with appropriate medium before use. Proliferation of the PaTu8988 cells is evaluated using CCK-8 assay. PaTu8988 cells are randomly into 4 groups and incubated in the absence or presence of concentrations of 0, 1.25, 2.5 and 5 μM) of Chidamide for 48 h. Subsequently, 10 μL CCK-8 is added in each well and incubated for 2 h. The optical density of each well is then measured with a microplate reader at 450 nm. The cell survival rate is calculated using the formula: Cell survival rate (%)=1-(ODctrl-ODsample)/ODctrl×100%
- 参考文献：
1. Zhao B, et al. Chidamide, a histone deacetylase inhibitor, functions as a tumor inhibitor by modulating the ratio of Bax/Bcl-2 and P21 in pancreatic cancer. Oncol Rep. 2015 Jan;33(1):304-10. 2.Chang Y Y, Wu H L, Fang H, et al. Comparison of three chemometric methods for processing HPLC-DAD data with time shifts: Simultaneous determination of ten molecular targeted anti-tumor drugs in different biological samples[J]. Talanta. 2021, 224: 121798. 3.Gong K, et al. CS055 (Chidamide/HBI-8000), a novel histone deacetylase inhibitor, induces G1 arrest, ROS-dependent apoptosis and differentiation in human leukaemia cells. Biochem J. 2012 May 1;443(3):735-46. 4.Ning ZQ, et al. Chidamide (CS055/HBI-82000): 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.
- 溶解性： Soluble in DMSO
- 保存条件： 2-8℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.561 ml 12.807 ml 25.614 ml 5 mM 0.512 ml 2.561 ml 5.123 ml 10 mM 0.256 ml 1.281 ml 2.561 ml 50 mM 0.051 ml 0.256 ml 0.512 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
