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。
| 生物活性 | GEM-5 is a gemcitabine-based conjugate containing aHIF-1αinhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression ofHIF-1αand up-regulate the expression of tumor suppressorp53. GEM-5 induces theapoptosisof A2780 cells and inhibits tumor growth[1]. |
| IC50& Target | IC50: 30 nM (HIF-1α) in A2780[1] |
体外研究
(In Vitro) | GEM-5 (0-80 μM; 12 hours) exhibits excellent antitumor activity toward A2780 cells under hypoxic condition with IC50of 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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体内研究
(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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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