EBI-2511

Catalog No.S8702 Batch:S870201

Technical Data

Formula	C₃₄H₄₈N₄O₄
Molecular Weight	576.77	CAS No.	2098546-05-3
Solubility (25°C)*	In vitro	Ethanol	13 mg/mL (22.53 mM)
		DMSO	3 mg/mL warmed with 50ºC water bath (5.2 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 AUC_0‑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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models Sprague Dawley rats and ICR mice 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.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
Sprague Dawley rats and ICR mice
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.

References

[1] Lu B, et al. ACS Med Chem Lett. 2018, 9(2):98-102.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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