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5-NIdR

Names

[ CAS No. ]:
191421-10-0

[ Name ]:
5-NIdR

Biological Activity

[Description]:

5-NIdR (1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole), an artificial nucleoside, exhibits the ability to inhibit the replication of DNA lesions generated by Temozolomide (HY-17364). 5-NIdR induces cancer cells apoptosis and arrests cell cycle at G0 phase. 5-NIdR enhances Temozolomide anti-tumor efficacy in murine glioblastoma model[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer

[In Vitro]

5-NIdR (12.5-100 μM;24-72 小时) 以剂量依赖性方式抑制人胶质母细胞瘤细胞系(U87、A172 和 SW1088)的生长[1]。 5-NIdR (1-100 μg/mL;72 h) 在 U87 细胞中诱导细胞凋亡,并以 100 μg/mL 的浓度过夜孵育,使细胞周期停滞在 G0 期[1]。

[In Vivo]

5-NIdR (100 mg/kg;腹腔注射;连续 5 天) 与替莫唑胺 (40 mg/kg) 联用,在胶质母细胞瘤小鼠异种移植模型中导致肿瘤完全消退。而 Temozolomide 单独使用,只能延迟肿瘤的生长[1]。

[References]

[1]. Choi JS, et al. Inhibition of Translesion DNA Synthesis as a Novel Therapeutic Strategy to Treat Brain Cancer. Cancer Res. 2018 Feb 15;78(4):1083-1096.  

Chemical & Physical Properties

[ Molecular Formula ]:
C13H14N2O5

[ Molecular Weight ]:
278.26100

[ Exact Mass ]:
278.09000

[ PSA ]:
100.44000

[ LogP ]:
1.71340


Related Compounds

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