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AS-0141 (Cdc7-IN-6) 是一种有效的 Cdc7 激酶抑制剂 (IC50=4 nM),具有抗肿瘤活性,详情请参考文献 WO2019165473A1,compound I-D。Cdc7 是一种丝氨酸苏氨酸蛋白激酶酶,在细胞周期中对 DNA 复制的启动至关重要。
AS-0141 (Cdc7-IN-6) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity[1][2].
AS-0141 (Cdc7-IN-6) demonstrates potent inhibitory activity (IC50<3 µμ) in a range of solid tumor cell lines, including those of bladder (5673, RT1 12/84), sarcoma (143B, CADO-ES1, RD-ES, A673), colon and cecum (Colo-205, DLD-l, LS1034, SK-CO-l, SNU-C1), renal (U0.31), head-and-neck (CNE-2Z, RPMI-2650), melanoma (A2058, A875), and gastric (HGC-27) lineages[1].
[1]. Christian Andrew HASSIG, et al. Methods of treatment of cancer comprising cdc7 inhibitors. WO2019165473A1.
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