货号	规格	价格	上海	北京	珠海	重庆	武汉
T19247-5mg	≥98%	￥1200.00 T19247-5mg ￥1200.00 3-5天	0 货期：3-5天	-	-	-	-
T19247-10mg	≥98%	￥1800.00 T19247-10mg ￥1800.00 3-5天	0 货期：3-5天	-	-	-	-
T19247-25mg	≥98%	￥3300.00 T19247-25mg ￥3300.00 3-5天	0 货期：3-5天	-	-	-	-
T19247-100mg	≥98%	￥5600.00 T19247-100mg ￥5600.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC50 of 6 nM

靶点：

IC50: 6 nM (CARM1);HistoneMethyltransferase

体外研究：

EZM 2302 binds to CARM1 and is a selective inhibitor of CARM1 activity (IC50=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 IC50 values in the nanomolar range (9, 31 nM, respectively). EZM 2302 inhibits the in vitro proliferation of multiple hematopoietic cell lines, with day 14 IC50 values of less than 100 nM in 9 of 15 cell lines。

体内研究：

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。

参考文献：

1. Drew AE, et al. Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma. Sci Rep. 2017 Dec 21;7(1):17993.

溶解性：

Soluble in DMSO

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.709 ml	8.546 ml	17.091 ml
5 mM	0.342 ml	1.709 ml	3.418 ml
10 mM	0.171 ml	0.855 ml	1.709 ml
50 mM	0.034 ml	0.171 ml	0.342 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

GSK 3359088

GSK3359088

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)