产品
编 号：F750181
分子式：C32H29F2N5O8
分子量：649.6
分子式：C32H29F2N5O8
分子量：649.6
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CAS No: 2233543-49-0
产品详情
生物活性：
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.
体内研究：
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.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.
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.
体外研究：
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.
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.
体内研究：
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.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.
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.
体外研究：
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.
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