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PROTAC EZH2 Degrader-1

Name: PROTAC EZH2 Degrader-1
Brand: TargetMol
SKU: T74602
Rating: 4.5 (1 reviews)

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Catalog No. T74602Cas No. 2641601-67-2

PROTAC EZH2 Degrader-1 (Compound 150d) is a potent PROTAC molecule that effectively suppresses EZH2 methyltransferase activity, with a half-maximal IC50 of 2.7 nM. EZH2 is a histone methyltransferase crucial to tumorigenesis and cancer progression, and PROTAC EZH2 Degrader-1 represents an important chemical tool for probing its therapeutic relevance.

PROTAC EZH2 Degrader-1

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Catalog No. T74602Cas No. 2641601-67-2

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$215	7-10 days	7-10 days
5 mg	$645	7-10 days	7-10 days
10 mg	$975	7-10 days	7-10 days

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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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Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	PROTAC EZH2 Degrader-1 (Compound 150d) is a potent PROTAC molecule that effectively suppresses EZH2 methyltransferase activity, with a half-maximal IC50 of 2.7 nM. EZH2 is a histone methyltransferase crucial to tumorigenesis and cancer progression, and PROTAC EZH2 Degrader-1 represents an important chemical tool for probing its therapeutic relevance.
Targets&IC50	EZH2:2.7 nM
In vitro	Methods: H128 cells were pretreated with PROTAC EZH2 Degrader-1 (2 nM), followed by treatment with carboplatin, etoposide, and teniposide for 72 hours. Cell viability was assessed using the CCK8 assay. Results: PROTAC EZH2 Degrader-1 significantly reduced the IC50 values of carboplatin, etoposide, and teniposide in H128-LM cells.[2]
In vivo	Methods: PROTAC EZH2 Degrader-1 (0.5 mg/kg, once weekly for a total of 3 doses) was administered intraperitoneally to H128-LM xenograft mice to evaluate tumor growth. Results: The combination of PROTAC EZH2 degrader-1 with carboplatin, etoposide, and teniposide significantly inhibited the growth of H128-LM tumors, demonstrating superior efficacy compared to chemotherapy drugs used alone.[2]

Chemical Properties

Molecular Weight	942.15
Formula	C₅₄H₆₇N₇O₈
Cas No.	2641601-67-2
Smiles	O=C(NCC=1C(=O)NC(=CC1C)C)C2=CC(=CC(=C2C)N(CC)C3CCOCC3)C4=CC=C(C=C4)CN5CCN(CC5)CCCCCCCOC6=CC=CC=7C(=O)N(C(=O)C67)C8C(=O)NC(=O)CC8

Storage & Solubility Information

Storage

keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (84.91 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.0614 mL	5.3070 mL	10.6140 mL	53.0701 mL
5 mM	0.2123 mL	1.0614 mL	2.1228 mL	10.6140 mL
10 mM	0.1061 mL	0.5307 mL	1.0614 mL	5.3070 mL
20 mM	0.0531 mL	0.2654 mL	0.5307 mL	2.6535 mL
50 mM	0.0212 mL	0.1061 mL	0.2123 mL	1.0614 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