GEM-5,2233543-49-0

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GEM-5

CAS No. : 2233543-49-0

MCE 国际站：GEM-5

产品活性：GEM-5 是一种基于吉西他滨、含有一个 HIF-1α 抑制剂 (YC-1) 的偶联物 (IC₅₀ = 30 nM)。GEM-5 能显著下调 HIF-1α 的表达，上调肿瘤抑制因子 p53 的表达。GEM-5 诱导 A2780 细胞凋亡 (apoptosis)，抑制肿瘤生长。

研究领域：Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：HIF/HIF Prolyl-Hydroxylase  |  Apoptosis  |  MDM-2/p53

In Vitro: GEM-5 (0-80 μM; 12 hours) exhibits excellent antitumor activity toward A2780 cells under hypoxic condition with IC₅₀ of 0.03 μM.
GEM-5 (0.5 μM; 72 hours) rises the apoptotic population to 52.67% under normoxic condition and 80.89% in A2780 cells under hypoxic condition.
GEM-5 (0.5 μM; 24 hours) arrests the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia).
GEM-5 (0.1 and 1 μM; 24 hours) decreases the levels of HIF-1α and increases the levels of p53 in a dose dependent manner under hypoxic condition.

In Vivo: GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity.

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