CAY10735

Anti-CSCs agent-1 is a potent anti-CSCs agent. Anti-CSCs agent-1 inhibits cell growth and cell migration. Anti-CSCs agent-1 induces apoptosis. Anti-CSCs agent-1 inhibits the viability of CSCs. Anti-CSCs agent-1 enhances the production of ROS in CSCs. Anti-CSCs agent-1 shows antitumor activity[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Anti-CSCs agent-1 (compound 48) (0, 0.25, 0.5 µM) 以剂量依赖性方式抑制 A375 和 B16F10 细胞的集落形成和细胞迁移[1]。 Anti-CSCs agent-1 (0, 1, 2, 3, 4 µM; 48 h) 诱导细胞凋亡，并以剂量依赖的方式增加 cleaved PARP、cleaved caspase-3、P-53 和 Bax 的表达[1]. Anti-CSCs agent-1 (0, 0.25, 0.5, 1.0, 2.0 µM; 24 h) 以剂量依赖的方式显着上调 E-cadherin 的表达来逆转上皮间质转化[1]. Anti-CSCs agent-1 (0-10 µM; 15 days) 抑制 CSCs 的活力，对球状体 A357、B16F10 细胞的 IC50 分别为 3.04、1.24[1]< /sup>. Anti-CSCs agent-1 (0-2 µM; 24 h) 以剂量依赖的方式显着增加 CSCs 中的 ROS 的产生[1]。 Cell Proliferation Assay[1] Cell Line: MDA-MB-231, 4T1, A375, B16F10, PANC-1, A549, LLC cells Concentration: 0-50 µM Incubation Time: 48 h Result: Showed antiproliferative activity with IC50s of 3.152, 0.7401, 0.8929, 0.6744, 1.107, 11.56, 0.9066 µM for MDA-MB-231, 4T1, A375, B16F10, PANC-1, A549, LLC cells, respectively. Apoptosis Analysis[1] Cell Line: A375, B16F10 cells Concentration: 0, 1, 2, 3 µM Incubation Time: 48 h Result: Induced cell apoptosis in a dose-dependen manner. Western Blot Analysis[1] Cell Line: A375, B16F10 cells Concentration: 0, 1, 2, 3, 4 µM Incubation Time: 48 h Result: Increased the expression of cleaved PARP, cleaved casepase-3, P-53 and Bax in a dose-dependent manner.

Anti-CSCs agent-1 (5 mg/kg; i.p.; daily for 15 days) 在小鼠体内显示出抗肿瘤活性[1]。 Animal Model: C57BL/6J mice (A375 cells)[1] Dosage: 5 mg/kg Administration: I.p.; daily for 15 days Result: Significantly inhibited tumor growth.

[1]. Liu X, et al. Synthesis and Discovery Novel Anti-Cancer Stem Cells Compounds Derived from the Natural Triterpenoic Acids. J Med Chem. 2018 Dec 13;61(23):10814-10833.