MS-275 (Entinostat) - CAS 209783-80-2
Catalog number:
209783-80-2
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Targets:
HDAC
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1. Histone deacetylase inhibitor entinostat in combination with a retinoid downregulates HER2 and reduces the tumor initiating cell population in aromatase inhibitor-resistant breast cancer
Amanda J. Schech, Preeti Shah,Stephen Yu. Breast Cancer Res Treat (2015) 152:499–508
Entinostat (ENT, MS-275, SNDX-275), a synthetic benzamide derivative class I histone deacetylase (HDAC) inhibitor, inhibits cell proliferation and promotes apoptosis in breast cancer. Previous studies from our laboratory have demonstrated that ENT reduces HER2 stability. We hypothesized that treatment of AI-resistant cells with ENT would inhibit the TIC population through downregulation of HER2. To further target the TIC population, we combined ENT with all-trans retinoic acid (ATRA), which is currently used to treat acute promyelocytic leukemia due to its regulation of differentiation, cell cycle control and apoptotic genes. We hypothesized that the combination of these two agents would provide dual inhibition of the TIC population.
2. A phase I study of the histone deacetylase (HDAC) inhibitor entinostat, in combination with sorafenib in patients with advanced solid tumors
Nuttapong Ngamphaiboon & Grace K. Dy & Wen Wee Ma & Yujie Zhao. Invest New Drugs (2015) 33:225–232
Entinostat (MS-275) is one of the most potent HDAC inhibitors in the class. Entinostat has been shown to inhibit HDACs by promoting hyperacetylation of nucleosomal histones. It is orally bioavailable and has a long half-life (approximately 52 h). A preclinical study demonstrated that entinostat induced apoptosis by activationof caspase-3, up-regulation of Bax and down-regulation of Bcl-2. Cell cycle was predominantly arrested at the G1/S checkpoint, which was associated with induction of the cyclin-dependent kinase inhibitor p21Waf/CIP1. A phase I study of entinostat in advanced solid tumors and lymphomas defined the maximal tolerated dose (MTD) of 10 mg/m2 orally every 14 days. Other dosing schedules have also been explored. Entinostat is well tolerated, and dose-limiting toxicities (DLTs) were described as nausea, vomiting, anorexia, and fatigue. Antitumor activity of single agent entinostat was limited. Thus, combinations of entinostat with other antitumor agents are currently being explored.
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CAS 209783-80-2 MS-275 (Entinostat)

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