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Home > Inhibitors & Agonists > Epigenetics > Histone Methyltransferase (HMTase)

EBI-2511

  Cat. No.:  DC11477   Featured
Chemical Structure
2098546-05-3
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More than 5000 active chemicals with high quality for research!
Field of application
EBI-2511 is a highly potent and orally active EZH2 inhibitor for the treatment of Non-Hodgkin’s Lymphoma.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2098546-05-3
Chemical Name: EBI-2511
Synonyms: EBI-2511;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;EBI2511;EBI 2511;4-Benzofurancarboxamide, 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]-
SMILES: O1C2=CC(N(CC)C3CCOCC3)=C(CC)C(C(NCC3=C(C)C=C(C)NC3=O)=O)=C2C=C1C1CCN(C(C)C)CC1
Formula: C34H48N4O4
M.Wt: 576.769329071045
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.
In Vivo: EBI-2511 displays a dose-dependent inhibition on the tumor growth, resulting in 28% (10mg/kg), 83% (30mg/kg), and 97% (100mg/kg) reduction in tumor size. At the same dosage level, EBI-2511 shows a superior anti-tumor efficacy to EPZ-6438 (P<0.01). It is noteworthy that no significant changes in body weights of all treatment groups are observed[1].
In Vitro: EBI-2511 (Compound 34) significantly reduces cellular H3K27me3 levels in a dose-dependent manner with an approximate IC50 of 8 nM, which is 3-fold more potent than EPZ-6438. In addition to Pfeffier cell line, EBI-2511 was shown active with IC50 value of 55 nM against WSU-DLCL2[1].
References: [1]. Lu B, et al. Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma. ACS Med Chem Lett. 2018 Jan 29;9(2):98-102.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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