WSF1-IN-1 (compound 136) 是具有口服活性的 WSF1 抑制剂，可用于Wolfram 综合征基因 WSF1 相关的肿瘤研究，其在HepG2 母源细胞系和 HepG2 WFS1 KO 细胞系中的 IC50 值分别为 0.33 μM 和>27 μM。
WSF1-IN-1 (compound 136), an orally active WSF1 inhibitor, can be used in the study for WSF1 (Wolfram syndrome) related tumors, with IC50 values of 0.33 μM and >27 μM in HepG2 parental and HepG2 WFS1 KO cell lines, respectively[1].
WSF1-IN-1 (compound 136) exhibits IC50 values of >27 μM and 0.03 μM for Hek293 empty vector and Hek293 WFS1 over-expressor, respectively. WSF1-IN-1 (compound 136) exhibits IC50 values of 0.05 μM (Colo-205 Control shRNA), >9 μM (Colo-205 WSF1 shRNA), 0.08 μM (DU4415 Control shRNA), 6.1 μM (DU4415 WSF1 shRNA), 0.26 μM (HepG2 Control shRNA), 2.2 μM (HepG2 WSF1 shRNA) for cell valiablity, respectively[1].
WSF1-IN-1 (compound 136, 100 mpk qd, orally, 14 days) exhibits 106.65% tumor growth inhibition (TGI) in NSCLC patient derived xenograft OD33996 nu/nu mice[1].
[1]. Lauffer, David J, et al. Preparation of pyridine compass. for the treatment of cellular proliferative disorders. US 20190322673 A1.
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