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EZH2-IN-4

Name: EZH2-IN-4
Brand: TargetMol
SKU: T39497
Rating: 4.5 (1 reviews)

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Catalog No. T39497Cas No. 2088132-99-2

Alias EZH2-IN-4

EZH2-IN-4 is a highly potent EZH2 inhibitor that can be taken orally. It exhibits inhibitory effects against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, with IC 50 values of 0.923 nM and 2.65 nM, respectively. Moreover, EZH2-IN-4 has demonstrated significant anti-cancer activity.

EZH2-IN-4

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Catalog No. T39497Alias EZH2-IN-4Cas No. 2088132-99-2

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
5 mg	$970	Inquiry	Inquiry

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	EZH2-IN-4 is a highly potent EZH2 inhibitor that can be taken orally. It exhibits inhibitory effects against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, with IC 50 values of 0.923 nM and 2.65 nM, respectively. Moreover, EZH2-IN-4 has demonstrated significant anti-cancer activity.
Targets&IC50	EZH2 (mutant 5-mer):2.65 nM (IC50), EZH2 (WT 5-mer):0.923 nM (IC50)
In vitro	EZH2-IN-4 (example 38) exhibits potent inhibition in Karpas-422 (EZH2 Y641N) cells with an H3K27me3 IC50 of 0.00973 nM and an IC50 of 10.1 nM in Plate Kj«pas-422 cells[1]. It suppresses the growth of various ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3), with IC50 values r ng ng from 0.02 to 8.6 μM, while show ng no inhibitory effect on SKOV3, HeyA8, and HEC59 cells (IC50 > 20 μM)[1].
In vivo	'EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) shows 73% inhibition of tumor methylation in the Karpas-422 xenograft model[1]. Additionally, administered twice daily at 50 mpk orally (po) with a 5-day pretreatment, followed by at least 23 days of concurrent administration with gemcitabine and cisplatin, it significantly inhibits tumor growth in the A2780 xenograft model[1].'
Synonyms	EZH2-IN-4

Chemical Properties

Molecular Weight	511.73
Formula	C₂₉H₄₁N₃O₃S
Cas No.	2088132-99-2
Smiles	[H][C@@]1(CC[C@@H](CC1)N1CC(C1)OC)[C@@H](C)c1sc2CCCN(Cc3c(C)cc(C)[nH]c3=O)C(=O)c2c1C \|wU:13.15,1.14,wD:4.7,1.0,(-2.14,-2.64,;-3.68,-2.64,;-2.91,-3.98,;-3.68,-5.31,;-5.22,-5.31,;-5.99,-3.98,;-5.22,-2.64,;-5.99,-6.64,;-5.59,-8.13,;-7.08,-8.53,;-7.48,-7.04,;-7.85,-9.86,;-9.39,-9.86,;-2.91,-1.31,;-3.68,.03,;-1.37,-1.31,;-.46,-.06,;1,-.54,;2.21,.42,;3.71,.08,;4.37,-1.31,;3.71,-2.7,;4.67,-3.9,;6.19,-3.67,;6.75,-2.24,;5.79,-1.03,;8.27,-2.01,;9.23,-3.21,;10.76,-2.98,;8.67,-4.65,;7.15,-4.87,;6.59,-6.31,;2.21,-3.04,;1.86,-4.54,;1,-2.08,;-.46,-2.55,;-.94,-4.02,)\|

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc