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CX-6258是口服活性的Pim 1,2和3激酶抑制剂,IC50为5 nM,25 nM和16 nM。
产品名称:
(3E)-5-氯-3-[[5-[3-[(六氢-4-甲基-1H-1,4-二氮杂卓-1-基)羰基]苯基]-2-呋喃基]亚甲基]-1,3-二氢-2H-吲哚-2-酮
物理化学性质:
溶解度: Insuluble (9.7E-3 g/L) (25 ºC),
密度: 1.309±0.06 g/cm3 (20 ºC 760 Torr)
[1]. Mustapha Haddach, Jerome Michaux, Michael K, Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med. Chem. Lett., 2012, 3 (2), pp 135-139
[2]. Padmanabhan A, Gosc EB, Bieberich CJ. Stabilization of the prostate-specific tumor suppressor NKX3.1 by the oncogenic protein kinase Pim-1 in prostate cancer cells. J Cell Biochem. 2013 May;114(5):1050-7.
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