(R)-BAY1238097 |
| رقم الكتالوجGC34443 |
(R) -BAY1238097 هو R-isomer مع نشاط أقل لـ BAY1238097BAY1238097 هو مثبط قوي وانتقائي لربط BET بالهيستونات وله نشاط قوي مضاد للتكاثر في نماذج مختلفة من AML (سرطان الدم النخاعي الحاد) ونماذج MM (المايلوما المتعددة) من خلال التنظيم السفلي لمستويات c-Myc ونسخة المصب
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Cas No.: 1564269-85-7
Sample solution is provided at 25 µL, 10mM.
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(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome[1][2]. BET[1].
[1]. Lejeune, P., et al. (2015) Abstract 3524: BAY 1238097, a novel BET inhibitor with strong efficacy in hematological tumor models. Cancer Research, 75(15 Suppl), 884. [2]. Bernasconi E, et al. Preclinical evaluation of the BET bromodomain inhibitor BAY 1238097 for the treatment of lymphoma. Br J Haematol. 2017 Sep;178(6):936-948.
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