中文名:EBI-2511
英文名:EBI-2511
纯度:Moligand™,≥98%
货号:E414124
Cas号:2098546-05-3
存储温度:-20°C储存
运输条件:超低温运输
产品介绍:
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
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关键字: 4-?Benzofurancarboxamid?e,N-?[(1,?2-?dihydro-?4,?6-?dimethyl-?2-?oxo-?3-?pyridinyl)?methyl]?-?5-?ethyl-?6-?[ethyl(tetrahydro-?2H-?pyran-?4-?yl)?amino]?-?2-?[1-?(1-?methylethyl)?-?4-?piperidinyl]?-
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