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JQEZ5

Catalog No.GC19211

JQEZ5 is a novel and potent EZH2 inhibitor.

Products are for research use only. Not for human use. We do not sell to patients.

JQEZ5 Chemical Structure

Cas No.: 1913252-04-6

Size Price Stock Qty
1mg
$43.00
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5mg
$84.00
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10mg
$144.00
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50mg
$540.00
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100mg
$945.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

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].

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.

Background

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.

Chemical Properties

Cas No. 1913252-04-6 SDF
Canonical SMILES CC(N1N=CC2=C(C(NCC3=C(C=C(NC3=O)C)CCC)=O)C=C(C4=CC=C(N=C4)N5CCN(C)CC5)N=C12)C
Formula C30H38N8O2 M.Wt 542.68
Solubility DMSO : 25 mg/mL (46.07 mM);Water : < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.8427 mL 9.2135 mL 18.4271 mL
5 mM 0.3685 mL 1.8427 mL 3.6854 mL
10 mM 0.1843 mL 0.9214 mL 1.8427 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 36 reference(s) in Google Scholar.)

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