PROTAC EZH2 Degrader-1

Cat. No.: HY-147525 Purity: 99.44%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC₅₀ of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes.

For research use only. We do not sell to patients.

PROTAC EZH2 Degrader-1 Chemical Structure

CAS No. : 2641601-67-2

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE PROTAC EZH2 Degrader-1

•BMC Cancer. 2024 Apr 22;24(1):504. [Abstract]

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

EZH2

2.7 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Pfeiffer	IC₅₀	0.21 μM Compound: E7	Antiproliferative activity against human Pfeiffer cells harboring EZH2-A677G mutant assessed as inhibition of cell growth incubated for 3 to 7 days by optical microscopic analysis (Rvb= 0.49 uM) Antiproliferative activity against human Pfeiffer cells harboring EZH2-A677G mutant assessed as inhibition of cell growth incubated for 3 to 7 days by optical microscopic analysis (Rvb= 0.49 uM)	[PMID: 33606537]
WSUDLCL2	IC₅₀	3.69 μM Compound: E7	Antiproliferative activity against human WSUDLCL2 cells harboring EZH2-Y641F mutant assessed as inhibition of cell growth incubated for 3 to 7 days by optical microscopic analysis (Rvb= 4.92 uM) Antiproliferative activity against human WSUDLCL2 cells harboring EZH2-Y641F mutant assessed as inhibition of cell growth incubated for 3 to 7 days by optical microscopic analysis (Rvb= 4.92 uM)	[PMID: 33606537]

Molecular Weight

942.15

Formula

C₅₄H₆₇N₇O₈

CAS No.

2641601-67-2

Appearance

Solid

Color

Off-white to light yellow

SMILES

CCN(C1CCOCC1)C2=C(C(C(NCC3=C(C=C(NC3=O)C)C)=O)=CC(C4=CC=C(C=C4)CN5CCN(CC5)CCCCCCCOC6=C7C(N(C(C7=CC=C6)=O)C8CCC(NC8=O)=O)=O)=C2)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (106.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0614 mL	5.3070 mL	10.6140 mL
5 mM	0.2123 mL	1.0614 mL	2.1228 mL
10 mM	0.1061 mL	0.5307 mL	1.0614 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.44%

Select Batch:

Data Sheet (271 KB) SDS (252 KB)

COA (247 KB) HNMR (298 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Juan Xia, et al. Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects. J Med Chem. 2022 May 26;65(10):7016-7043. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.0614 mL	5.3070 mL	10.6140 mL	26.5351 mL
	5 mM	0.2123 mL	1.0614 mL	2.1228 mL	5.3070 mL
	10 mM	0.1061 mL	0.5307 mL	1.0614 mL	2.6535 mL
	15 mM	0.0708 mL	0.3538 mL	0.7076 mL	1.7690 mL
	20 mM	0.0531 mL	0.2654 mL	0.5307 mL	1.3268 mL
	25 mM	0.0425 mL	0.2123 mL	0.4246 mL	1.0614 mL
	30 mM	0.0354 mL	0.1769 mL	0.3538 mL	0.8845 mL
	40 mM	0.0265 mL	0.1327 mL	0.2654 mL	0.6634 mL
	50 mM	0.0212 mL	0.1061 mL	0.2123 mL	0.5307 mL
	60 mM	0.0177 mL	0.0885 mL	0.1769 mL	0.4423 mL
	80 mM	0.0133 mL	0.0663 mL	0.1327 mL	0.3317 mL
	100 mM	0.0106 mL	0.0531 mL	0.1061 mL	0.2654 mL