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EBI-2511 - 98%, high purity , CAS No.2098546-05-3, Inhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit

  • Moligand™
  • ≥98%
Item Number
E414124
Grouped product items
SKUSizeAvailabilityPrice Qty
E414124-1mg
1mg
In stock
$42.90
E414124-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$177.90
E414124-10mg
10mg
In stock
$276.90
E414124-25mg
25mg
In stock
$573.90
E414124-50mg
50mg
In stock
$840.90
E414124-100mg
100mg
In stock
$1,335.90
E414124-250mg
250mg
In stock
$3,006.90

EZH1/2 Inhibitors

Basic Description

Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsEBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G).
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit
Product Description

Information

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


Targets

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 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.


Cell Research(from reference)

Cell lines:Pfeiffer cells 

Incubation Time:5 days 

Product Properties

ALogP4.484
HBD Count2
Rotatable Bond9

Associated Targets

EZH1 Tchem Histone-lysine N-methyltransferase EZH1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EZH2 Tclin Histone-lysine N-methyltransferase EZH2 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-5-ethyl-6-[ethyl(oxan-4-yl)amino]-2-(1-propan-2-ylpiperidin-4-yl)-1-benzofuran-4-carboxamide
INCHI InChI=1S/C34H48N4O4/c1-7-26-29(38(8-2)25-11-15-41-16-12-25)19-31-27(18-30(42-31)24-9-13-37(14-10-24)21(3)4)32(26)34(40)35-20-28-22(5)17-23(6)36-33(28)39/h17-19,21,24-25H,7-16,20H2,1-6H3,(H,35,40)(H,36,39)
InChi Key NYWVSLBALKNFJR-UHFFFAOYSA-N
Canonical 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
Isomeric 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
PubChem CID 133081962
Molecular Weight 576.77

Certificates

Certificate of Analysis(COA)

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6 results found

Lot NumberCertificate TypeDateItem
K2217741Certificate of AnalysisAug 17, 2022 E414124
K2217743Certificate of AnalysisAug 17, 2022 E414124
K2217762Certificate of AnalysisAug 17, 2022 E414124
K2217785Certificate of AnalysisAug 17, 2022 E414124
K2217817Certificate of AnalysisAug 17, 2022 E414124
K2217818Certificate of AnalysisAug 17, 2022 E414124

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 30 mg/mL (52.01 mM); Ethanol: 13 mg/mL (22.53 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility30
DMSO(mM) Max Solubility52.0138009951974
Water(mg / mL) Max Solubility<1

Related Documents

References

1. Lu B, Shen X, Zhang L, Liu D, Zhang C, Cao J, Shen R, Zhang J, Wang D, Wan H et al..  (2018)  Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma..  ACS Med Chem Lett,  (2): (98-102).  [PMID:29456795]

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