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EZM0414

Name: EZM0414
Brand: TargetMol
SKU: T9969
Price: 279 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9969Cas No. 2411748-50-8

Alias SETD2-IN-1

EZM0414 is a potent and selective, orally bioavailable inhibitor of SETD2 with an IC50 of 18 nM in biochemical assays and 34 nM in cellular assays, potentially useful for researching relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma [1].

EZM0414

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Purity: 99.58%

Catalog No. T9969Alias SETD2-IN-1Cas No. 2411748-50-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$279	In Stock	In Stock
5 mg	$688	In Stock	In Stock
10 mg	$978	In Stock	In Stock
25 mg	$1,460	In Stock	In Stock
50 mg	$1,960	In Stock	In Stock
100 mg	$2,650	In Stock	In Stock

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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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Purity:99.58%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

EZM0414 AI Summary

EZM0414 demonstrates notable bioactivities including potent inhibition of SETD2 with low IC50 values across various assays. It exhibits significant antiproliferative effects against human cancer cell lines KMS-34 and KMS-11, reducing cell viability. The compound also shows good permeability across Caco-2 cells, indicating potential for absorption and promising pharmacokinetic properties such as oral bioavailability and acceptable half-life values in animal models. Stability tests reveal that it has moderate to high clearance rates in hepatocytes from different species. Additionally, EZM0414 functions as a D2 receptor antagonist and a 5-HT1B receptor agonist. In vivo, it demonstrates a significant antitumor effect in xenografted mouse models with KMS-11 cells, effectively reducing tumor growth. These properties suggest that EZM0414 could be a viable candidate for cancer treatment..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	EZM0414 is a potent and selective, orally bioavailable inhibitor of SETD2 with an IC50 of 18 nM in biochemical assays and 34 nM in cellular assays, potentially useful for researching relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma [1].
Synonyms	SETD2-IN-1

Chemical Properties

Molecular Weight	400.49
Formula	C₂₂H₂₉FN₄O₂
Cas No.	2411748-50-8
Smiles	[H][C@@]1(CCC[C@H](C1)NC(=O)c1cc2c(F)ccc(C)c2[nH]1)N1CCN(CC1)C(C)=O

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.

Solubility Information

DMSO: 50 mg/mL (124.85 mM), Sonication and heating to 60℃ are recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4969 mL	12.4847 mL	24.9694 mL	124.8471 mL
5 mM	0.4994 mL	2.4969 mL	4.9939 mL	24.9694 mL
10 mM	0.2497 mL	1.2485 mL	2.4969 mL	12.4847 mL
20 mM	0.1248 mL	0.6242 mL	1.2485 mL	6.2424 mL
50 mM	0.0499 mL	0.2497 mL	0.4994 mL	2.4969 mL
100 mM	0.0250 mL	0.1248 mL	0.2497 mL	1.2485 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