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JQEZ5
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。
JQEZ5图片
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
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100mg电议

产品介绍
JQEZ5 是一种有效的选择性 EZH2 赖氨酸甲基转移酶抑制剂。 JQEZ5 SAM 竞争性抑制多梳抑制复合物 2 (PRC2),IC50 为 80 nM。 JQEZ5具有抗肿瘤作用。

Animal experiment:

Tumor-bearing genetically-engineered mouse models (GEMMs) are monitored for onset of symptoms (breath distress) and then treated with JQEZ5 for three weeks (75 mg/kg IP daily). Tumors are visualized by MRI and tumor volume of the lungs is calculated using 3D Slicer. For xenograft experiments, H661 cells are dissociated into single cells, counted and resuspended at 2×106 cells per 250 μL of 1:1 media/matrigel. Eight- to 12-week-old female Foxn1nu/Foxn1nu mice are injected subcutaneously with 2×106 cells in two to three spots on the flanks. Tumors are allowed to grow to an approximate size of 200 mm3 (~10 weeks) and the mice are randomized for vehicle (n=3) or JQEZ5 administration (n=6, 75 mg/kg/d, i.p.) for 18 days. Tumor growth is measured by caliper measurements and tumor volume is calculated by standard methods[1].

产品描述

JQEZ5 is a novel and potent EZH2 inhibitor.

Animals treated with JQEZ5 exhibit rapid and pronounced tumor regression over the three week treatment course. H3K27me3 levels are largely reduced with treatment further confirming the on-target effect of JQEZ5 in mice. The level of H3K27me3 is largely reduced with the treatment without effect on EZH2 levels in both the tumor and in the lung tissue of JQEZ5 treated animals[1].

References:
[1]. Zhang H, et al. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016 Sep;6(9):1006-21.