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GEM-5
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GEM-5图片
CAS NO:2233543-49-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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
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.
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.