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CCT244747 是一种有效的,可口服的,高度选择性的 CHK1 抑制剂,IC50 值为 7.7 nM;CCT244747 可废除 G2 检查点,IC50 值为 29 nM。
中文名称:
3-[(1R)-2-(二甲基氨基)-1-甲基乙氧基]-5-[[4-甲氧基-5-(1-甲基-1H-吡唑-4-基)-2-吡啶基]氨基]-2-吡嗪甲腈
[1]. Lainchbury M, et al. Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. J Med Chem. 2012 Nov 26;55(22):10229-40.
[2]. Walton MI, et al. CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs. Clin Cancer Res. 2012 Oct 15;18(20):5650-61.
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