EZM 2302

Name: EZM 2302
Brand: MedChemExpress
SKU: HY-111109
Rating: 5.0 (9 reviews)

Cat. No.: HY-111109 Purity: 99.59%: FAQs
Data Sheet SDS COA Handling Instructions

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EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC₅₀ of 6 nM.

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

EZM 2302 Chemical Structure

CAS No. : 1628830-21-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 257	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 257	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 580	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 9 publication(s) in Google Scholar

8 Publications Citing Use of MCE EZM 2302

: EZM 2302 purchased from MedChemExpress. Usage Cited in: Aging (Albany NY). 2020 Jun 2;12(11):10578-10593. [Abstract]; The Western blot results show that EZM2302 (10 nM) inhibits the enzymatic activity of CARM1 and CARM2, leading to significantly reduced H3R17me2a and H3R26me2a levels.

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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
Protocol
Purity & Documentation
References
Customer Review

Description

EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC₅₀ of 6 nM.

IC₅₀ & Target

IC50: 6 nM (CARM1)^[1]

In Vitro

EZM 2302 binds to CARM1 and is a selective inhibitor of CARM1 activity (IC₅₀=6 nM) with broad selectivity against other histone methyltransferases. Treatment of MM cell lines with EZM 2302 leads to inhibition of PABP1 and SMB methylation and cell stasis with IC₅₀ values in the nanomolar range (9, 31 nM, respectively). EZM 2302 inhibits the in vitro proliferation of multiple hematopoietic cell lines, with day 14 IC₅₀ values of less than 100 nM in 9 of 15 cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

EZM 2302 is stable in human hepatocytes (CL<3 mL/min/kg), and moderately binds to human, mouse and rat plasma proteins with a mean fraction unbound of 0.66, 0.46 and 0.74, respectively. In mouse and rat, the plasma clearance (CL) is 43 and 91 mL/min/kg, respectively. EZM 2302 shows dose-dependent exposure and tumor growth inhibition (TGI) after 21 days in the RPMI-8226 xenograft model. Tumors in all EZM 2302 dose groups measured on day 21 show significant decreases in tumor growth compared to vehicle^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

585.09

Formula

C₂₉H₃₇ClN₆O₅

CAS No.

1628830-21-6

Appearance

Solid

Color

White to off-white

SMILES

CNC[C@@H](O)COC1=CC=C(Cl)C(C2=NC(N3CC4(CCN(C(OC)=O)CC4)C3)=C(C)C(C5=C(C)ON=C5C)=N2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (170.91 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	1.7091 mL	8.5457 mL	17.0914 mL
5 mM	0.3418 mL	1.7091 mL	3.4183 mL
10 mM	0.1709 mL	0.8546 mL	1.7091 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.59%

Select Batch:

Data Sheet (278 KB) SDS (392 KB)

COA (249 KB) LCMS (99 KB)

Handling Instructions (2659 KB)

References

[1]. Drew AE, et al. Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma. Sci Rep. 2017 Dec 21;7(1):17993. [Content Brief]

Cell Assay ^[1]	Cultured cells in linear/log phase growth are split to a seeding density of 2e5 cells/mL in 2–20mLs of media, depending on the yield required at the end of the growth period. EZM 2302 is diluted in DMSO and added to each culture vessel with a final DMSO concentration of 0.2%. Cells are allowed to grow for 96 hours. At the conclusion of each treatment period, cells are harvested by centrifugation (5 minutes, 1200 rpm), and cell pellets are rinsed once with PBS before being frozen on dry ice pending further processing^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Rats^[1] Male Sprague-Dawley rats (n=3) are treated with a single dose of EZM2302 at 2 mg/kg by intravenous (i.v.) injection and 10 mg/kg by oral gavage administration (p.o.; mouse only), formulated in 5% dextrose in water, pH 3.5. An additional group of rats, cannulated in both the jugular and portal veins are dosed by oral gavage (10 mg/kg, in 0.5% methylcellulose in water). Approximately 110 μL of blood is taken from the animals by retro-orbital bleeding (mouse), tail vein (rat i.v.) or both jugular and portal vein sampling (rat p.o.) at pre-specified time intervals. The 2 h samples are split for parallel determination of blood and plasma concentration^[1]. Mice^[1] RPMI-8226 cells are inoculated at 5×10⁶ cells/mouse and treatment began when the mean tumor sizes reach 120 mm³ (28 days post-inoculation). CB-17 SCID Mice are assigned into groups using a randomized block design. EZM2302 or vehicle (0.5% methylcellulose in water) is administered orally BID at a dose volume of 37.5, 75, 150, or 300 mg/kg for 21 days. Body weights are measured twice a week for the duration of the study. Tumor size is measured twice weekly in two dimensions using a caliper, and the volume is expressed in cubic millimeters. Animals are euthanized 3 hours post-final dose, with blood and tissues collected for analysis^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Drew AE, et al. Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma. Sci Rep. 2017 Dec 21;7(1):17993. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.7091 mL	8.5457 mL	17.0914 mL	42.7285 mL
	5 mM	0.3418 mL	1.7091 mL	3.4183 mL	8.5457 mL
	10 mM	0.1709 mL	0.8546 mL	1.7091 mL	4.2728 mL
	15 mM	0.1139 mL	0.5697 mL	1.1394 mL	2.8486 mL
	20 mM	0.0855 mL	0.4273 mL	0.8546 mL	2.1364 mL
	25 mM	0.0684 mL	0.3418 mL	0.6837 mL	1.7091 mL
	30 mM	0.0570 mL	0.2849 mL	0.5697 mL	1.4243 mL
	40 mM	0.0427 mL	0.2136 mL	0.4273 mL	1.0682 mL
	50 mM	0.0342 mL	0.1709 mL	0.3418 mL	0.8546 mL
	60 mM	0.0285 mL	0.1424 mL	0.2849 mL	0.7121 mL
	80 mM	0.0214 mL	0.1068 mL	0.2136 mL	0.5341 mL
	100 mM	0.0171 mL	0.0855 mL	0.1709 mL	0.4273 mL

EZM 2302 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EZM 23021628830-21-6EZM2302EZM-2302Histone MethyltransferaseInhibitorinhibitorinhibit

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EZM 2302

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EZM 2302 Related Antibodies

8 Publications Citing Use of MCE EZM 2302

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•Related Screening Libraries:

•Related Small Molecules:

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View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

EZM 2302 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

EZM 2302 Related Classifications

Keywords:

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