EBI-2511

Catalog No.S8702

EBI-2511 Chemical Structure

Molecular Weight(MW): 576.77

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

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Purity & Quality Control

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Biological Activity

Description EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G).
Targets
EZH2(A667G) [1]
(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 EBI-2511 (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 EBI-2511 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 EBI-2511 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 EBI-2511 in human, rat, and mouse are 93.9%, 94.0%, and 92.7%, respectively[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: Pfeiffer cells
  • Concentrations: --
  • Incubation Time: 5 days
  • Method:

    Cells are seeded in 96 well plates at a density of 1,000 to 8,000 cells per well and cultured overnight at 37 ℃ incubator in medium supplemented with 10% FBS. On the next day, the test compounds at various concentrations or vehicle control (0.5% DMSO) are added into cell culture. After 5 day treatment, the growth of cells is evaluated.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Sprague Dawley rats and ICR mice
  • Formulation: 0.5% CMC Na and 0.1% Tween 80 for p.o and solution in the mixtures of Dimethylacetamide and Propylene Glycol for i.v.
  • Dosages: In rats: 5 mg/kg (p.o.), 0.5 mg/kg (i.v.); In mice, 10 mg/kg (p.o.), 1 mg/kg (i.v.)
  • Administration: i.v. or p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 30 mg/mL (52.01 mM)
Ethanol 13 mg/mL (22.53 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 576.77
Formula

C34H48N4O4

CAS No. 2098546-05-3
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID