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(S)-Crizotinib

CAS No. : 1374356-45-2

MCE 站：(S)-Crizotinib

产品活性：(S)-Crizotinib 是一种有效的选择性 MTH1 (mutT 同源物)抑制剂，IC₅₀ 为 330 nM。(S)-Crizotinib 通过抑制 MTH1 破坏核苷酸库的稳态，诱导 DNA 单链断裂的增加，激活人结肠癌细胞的 DNA 修复，并有效抑制动物模型中的肿瘤生长。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：DNA/RNA Synthesis  |  Apoptosis

In Vitro: (S)-crizotinib (0.625-80 μM; 24 hours) decreases the viability of NCI-H460, H1975 and A549 cells with IC₅₀ values of 14.29, 16.54 and 11.25 μM, respectively.
(S)-crizotinib (10-30 μM; 24 hours) induces NCI-H460, H1975 and A549 cells apoptosis.
(S)-crizotinib (10-30 μM; 24 hours) decreases Bcl-2: Bax ratio. (S)-crizotinib decreases B cell lymphoma 2 (Bcl-2), and Bcl-2 associated protein x (Bax) is either unaltered (H460 cells) or shows an increase (H1975 cells).
(S)-Crizotinib induces apoptosis in human non-small cell lung cancer (NSCLC) cells by activating ROS-dependent ER stress apoptotic pathway independent of mutT homologue (MTH1).

In Vivo: (S)-crizotinib (7.5 or 15 mg/kg; intraperitoneal injections; once daily for 10 days) results in significant reductions in both tumor volume and tumor weight.

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