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EEDi-5285

Name: EEDi-5285
Brand: TargetMol
SKU: T22322
Rating: 4.5 (1 reviews)

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Catalog No. T22322Cas No. 2488952-40-3

Alias UM-EEDi-5285, EEDI5285

EEDi-5285, an orally active and highly potent inhibitor targeting embryonic ectoderm development (EED) protein, exhibits anti-cancer activity. It demonstrates exceptional efficacy with an IC50 value of 0.2 nM, indicating robust binding affinity to the EED protein.

EEDi-5285

😃Good

Catalog No. T22322Alias UM-EEDi-5285, EEDI5285Cas No. 2488952-40-3

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$3,000	Inquiry	Inquiry
10 mg	$4,500	Inquiry	Inquiry
25 mg	$7,300	Inquiry	Inquiry
50 mg	$11,000	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$3,400	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	EEDi-5285, an orally active and highly potent inhibitor targeting embryonic ectoderm development (EED) protein, exhibits anti-cancer activity. It demonstrates exceptional efficacy with an IC50 value of 0.2 nM, indicating robust binding affinity to the EED protein.
Targets&IC50	EED:0.2 nM (IC50)
In vitro	EEDi-5285 effectively suppresses cell proliferation in lymphoma cell lines Pfeiffer and KARPAS422, which possess an EZH2 mutation, demonstrating inhibition concentrations (IC50) of 20 pM and 0.5 nM, respectively[1].
In vivo	EEDi-5285 (compound 28; 50-100 mg/kg; oral gavage; daily; for 28 days; SCID mice) treatment results in complete and durable tumor regression in the KARPAS422 xenograft model. A single 100 mg/kg oral dose reduces H3K27me3 levels at 24 h in KARPAS422 tumor tissue. The compound achieves a Cmax of 1.8 μM, an AUC of 6.0 h▪μg/ml with 10 mg/kg orally, and an oral bioavailability (F) of 75%. It has a moderate volume of distribution of 1.4 L/kg and a terminal T1/2 of approximately 2 h[1].
Synonyms	UM-EEDi-5285, EEDI5285

Chemical Properties

Molecular Weight	479.53
Formula	C₂₄H₂₂FN₅O₃S
Cas No.	2488952-40-3
Smiles	CS(=O)(=O)c1ncn2c(NCc3c4CCOc4ccc3F)ncc(-c3ccc(nc3)C3CC3)c12
Relative Density.	1.56 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from direct sunlight | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 112.5 mg/mL (234.6 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0854 mL	10.4269 mL	20.8538 mL	104.2688 mL
5 mM	0.4171 mL	2.0854 mL	4.1708 mL	20.8538 mL
10 mM	0.2085 mL	1.0427 mL	2.0854 mL	10.4269 mL
20 mM	0.1043 mL	0.5213 mL	1.0427 mL	5.2134 mL
50 mM	0.0417 mL	0.2085 mL	0.4171 mL	2.0854 mL
100 mM	0.0209 mL	0.1043 mL	0.2085 mL	1.0427 mL

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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