EZM 2302

CAS: 1628830-21-6 货号: E655335 分子式: C29H37ClN6O5 分子量: 585.09
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
E655335-1ml
期货 Stock Image
¥1,999.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 ( CARM1 ) with an IC 50 of 6 nM.

In Vitro

EZM 2302 binds to CARM1 and is a selective inhibitor of CARM1 activity (IC 50 =6 nM) with broad selectivity against other histone methyltransferases. Treatment of MM cell lines with EZM 2302 leads to inhibition of PABP1 and SMB methylation and cell stasis with IC 50 values in the nanomolar range (9, 31 nM, respectively). EZM 2302 inhibits the in vitro proliferation of multiple hematopoietic cell lines, with day 14 IC 50 values of less than 100 nM in 9 of 15 cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

EZM 2302 is stable in human hepatocytes (CL<3 mL/min/kg), and moderately binds to human, mouse and rat plasma proteins with a mean fraction unbound of 0.66, 0.46 and 0.74, respectively. In mouse and rat, the plasma clearance (CL) is 43 and 91 mL/min/kg, respectively. EZM 2302 shows dose-dependent exposure and tumor growth inhibition (TGI) after 21 days in the RPMI-8226 xenograft model. Tumors in all EZM 2302 dose groups measured on day 21 show significant decreases in tumor growth compared to vehicle . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:IC50: 6 nM (CARM1)

规格

规格或纯度
10mM in DMSO
英文名称
EZM 2302
生化机理
EZM 2302 是辅激活剂相关精氨酸甲基转移酶 1(CARM1)的抑制剂,IC50 为 6u2009nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=C(N=C(N=C1N2CC3(C2)CCN(CC3)C(=O)OC)C4=C(C=CC(=C4)OC[C@@H](CNC)O)Cl)C5=C(ON=C5C)C
分子量
585.09

技术文档

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🔬 规格说明书

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高级数据

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