EBI-2511|2098546-05-3|-陌孚医药/Medlife

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EBI-2511

目录号: PL15026 纯度: ≥99%

CAS No. :2098546-05-3

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中文名称	EBI-2511
中文别名	化合物EBI-2511
英文名称	EBI-2511
英文别名	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]-
Cas No.	2098546-05-3
分子式	C₃₄H₄₈N₄O₄
分子量	576.77
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	EBI-2511 是具有口服活性的、EZH2 的有效抑制剂，其在 Pfeffiera 细胞中的 IC₅₀ 值为6 nM。
生物活性	EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC 50 of 6 nM in Pfeffiera cell lines, respectively.
性状	Solid
IC50 & Target[1][2]	IC50: 6 nM (EZH2).
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Lu B, et al. Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkins Lymphoma. ACS Med Chem Lett. 2018 Jan 29;9(2):98-102.

溶解度数据	In Vitro: DMSO : 5 mg/mL (8.67 mM; Need ultrasonic)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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