產品名稱：Mocetinostat, Free Base 產品貨號：LC M-2433 產品規(guī)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
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