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LY-364947 是一种有效的,ATP 竞争性的 TGFβR-I 抑制剂,IC50 值为 59 nM,是对 TGFβR-II 选择性的 7 倍。
中文别名:
4-(3-吡啶-2-基-1H-吡唑-4-基)喹啉;
4-[3-(2-吡啶基)-1H-吡唑-4-基]喹啉;
4-[3-(2-吡啶基)-1H-吡唑-4-基]喹啉
物化属性:
密度:1.283
沸点:490.8°C at 760 mmHg
折射率:1.7
闪光点:268.7°C
PSA:54.46000
LOGP:3.68690
[1]. Peng SB, et al. Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition. Biochemistry, 2005, 44(7), 2293-2304.
[2]. Oka M, et al. Inhibition of endogenous TGF-beta signaling enhances lymphangiogenesis. Blood, 2008, 111(9), 4571-4579.
[3]. Naka K, et al. TGF-beta-FOXO signalling maintains leukaemia-initiating cells in chronic myeloid leukaemia. Nature, 2010, 463(7281), 676-680.
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