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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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E422546-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $667.90 |
EZH1/2 Inhibitors
Specifications & Purity | Moligand™, 10mM in DMSO |
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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 -80°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
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 |
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DMSO(mg / mL) Max Solubility | 30 |
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DMSO(mM) Max Solubility | 52.0138009951974 |
Water(mg / mL) Max Solubility | <1 |