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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	Availability
1 mg	$215	7-10 days
5 mg	$645	7-10 days
10 mg	$975	7-10 days

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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
Color	White
Appearance	Solid

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

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DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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