Home Methylation EZH2 inhibitor EBI-2511

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EBI-2511 EZH2 inhibitor

Cat.No.S8702

EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G).
EBI-2511 EZH2 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 576.77

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Quality Control

Batch: S870201 Ethanol]13 mg/mL]false]DMSO]3 mg/mL]true]Water]Insoluble]false Purity: 99.88%
99.88

Solubility

In vitro
Batch:

Ethanol : 13 mg/mL

DMSO : 3 mg/mL (5.2 mM) Warmed with 50°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 576.77 Formula

C34H48N4O4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2098546-05-3 -- Storage of Stock Solutions

Synonyms N/A Smiles CCC1=C(C2=C(C=C1N(CC)C3CCOCC3)OC(=C2)C4CCN(CC4)C(C)C)C(=O)NCC5=C(C=C(NC5=O)C)C

Mechanism of Action

Targets/IC50/Ki
EZH2(A667G)
(Cell-free assay)
4 nM
In vivo

In in vivo experiments, rats are administrated with dosages of 5 mg/kg EBI-2511 (p.o.) and 0.5 mg/kg this compound (i.v.). Mice are administrated with dosages of 10 mg/kg p.o. and 1.0 mg/kg i.v. For i.v. administration, the clearance of this compound is modest with CLz/F of 26 and 32 mL/min/kg in rats and mice, respectively. After a single 5 and 10 mg/kg oral dose of a CMC-Na suspension of this chemical to rats and mice, its AUC0‑t reaches 239 and 774 ng/mL·h with oral bioavailability of 9% and 16%, respectively. plasma protein binding of this compound in human, rat, and mouse are 93.9%, 94.0%, and 92.7%, respectively.
References

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