Mocetinostat, Free Base **

产品名称：Mocetinostat, Free Base
产品货号：LC  M-2433 
产品规格：100 MG
Mocetinostat selectively inhibits histone deacetylases (HDACs) 1-3 and 11 at submicromolar concentrations.  It blocks cancer cell proliferation in vitro and has significant antitumor activity in vivo.  Zhou, N., et al.  "Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor."  J. Med. Chem. 51:  4072-4075 (2008).
Mocetinostat induces hyperacetylation of histones, causes expression of the tumor suppressor protein p21(WAF1/CIP1), and inhibits proliferation of human cancer cells growing in culture.  Raeppel, S., et al.  "SAR and biological evaluation of analogues of a small molecule histone deacetylase inhibitor N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide (MGCD0103)."  Bioorg. Med. Chem. Lett. 19:  644-649 (2009).
Mocetinostat demonstrated antitumor activity against hematological and lymphoproliferative cancers.  Le Tourneau, C. and Siu, L.L.  "Promising antitumor activity with MGCD0103, a novel isotype-selective histone deacetylase inhibitor."  Expert Opin. Investig. Drugs 17:  1247-1254 (2008).
Mocetinostat dose-dependently inhibited HDAC activity in several human cancer cell lines and in human peripheral white blood cells.  The inhibitory effect of mocetinostat lasted for at least 8 hours in mice and 48 hours in patients with solid tumors.  Bonfils, C., et al.  "Evaluation of the pharmacodynamic effects of MGCD0103 from preclinical models to human using a novel HDAC enzyme assay."  Clin. Cancer Res. 14:  3441-3449 (2008).
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO.  Disposal:  A

产品留言

标题

联系人

联系电话

内容

验证码

点击换一张

注：1.可以使用快捷键Alt+S或Ctrl+Enter发送信息!
2.如有必要,请您留下您的详细联系方式!