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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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
Specifications & Purity | Moligand™, ≥98% |
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Biochemical and Physiological Mechanisms | EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G). |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor 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 |
ALogP | 4.484 |
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HBD Count | 2 |
Rotatable Bond | 9 |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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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 |
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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 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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K2217741 | Certificate of Analysis | Aug 17, 2022 | E414124 |
K2217743 | Certificate of Analysis | Aug 17, 2022 | E414124 |
K2217762 | Certificate of Analysis | Aug 17, 2022 | E414124 |
K2217785 | Certificate of Analysis | Aug 17, 2022 | E414124 |
K2217817 | Certificate of Analysis | Aug 17, 2022 | E414124 |
K2217818 | Certificate of Analysis | Aug 17, 2022 | E414124 |
Solubility | Solubility (25°C) In vitro DMSO: 30 mg/mL (52.01 mM); Ethanol: 13 mg/mL (22.53 mM); Water: Insoluble; |
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DMSO(mg / mL) Max Solubility | 30 |
DMSO(mM) Max Solubility | 52.0138009951974 |
Water(mg / mL) Max Solubility | <1 |
Starting at $667.90
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, 9 (2): (98-102). [PMID:29456795] |