GEM-5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GEM-5 

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。

GEM-5

GEM-5 Chemical Structure

CAS No. : 2233543-49-0

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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[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 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

649.60

Formula

C32H29F2N5O8
CAS 号

2233543-49-0
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.
参考文献

  • [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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