| Description |
GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth[1].
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| Related Catalog |
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| Target |
IC50: 30 nM (HIF-1α) in A2780[1]
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| 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[1]. 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[1]. GEM-5 (0.5 μM; 24 hours) arrests the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia)[1]. 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[1]. Apoptosis Analysis Cell Line: A2780 cells[1] Concentration: 0.5 μM Incubation Time: 72 hours Result: Rose the apoptotic population to 52.67% under normoxic condition and 80.89% under hypoxic condition. Cell Cycle Analysis Cell Line: A2780 cells[1] Concentration: 0.5 μM Incubation Time: 24 hours Result: Arrested the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia). Western Blot Analysis Cell Line: A2780 cells[1] Concentration: 0.1 and 1 μM Incubation Time: 24 hours Result: Decreased the levels of HIF-1α and increased the levels of p53 in a dose dependent manner
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| 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[1]. Animal Model: 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[1]. Dosage: 125 or 271 mg/kg Administration: Tail vein injection, once a week for 4 weeks Result: Effectively inhibited tumor growth in the A2780 xenograft mouse model and exhibited low toxicity.
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| References |
[1]. Xu Z, et al. A gemcitabine-based conjugate with enhanced antitumor efficacy by suppressing HIF-1α expression under hypoxia. Bioorg Med Chem. 2021;41:116214.
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