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EZM 2302

产品编号 T5605 CAS 1628830-21-6

别名: GSK3359088

EZM 2302 (GSK3359088) 是选择性口服精氨酸甲基转移酶 CARM1 抑制剂，IC50值为 6 nM。

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EZM 2302, CAS 1628830-21-6

规格	价格/CNY	货期
1 mg	￥ 612	现货
2 mg	￥ 857	现货
5 mg	￥ 1,330	现货
10 mg	￥ 1,980	现货
25 mg	￥ 3,380	现货
50 mg	￥ 4,850	现货
100 mg	￥ 6,760	现货
500 mg	￥ 13,500	现货
1 mL * 10 mM (in DMSO)	￥ 1,730	现货

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选择批次

纯度: 98%

纯度: 97.47%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	EZM 2302 (GSK3359088) is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).
靶点活性	CARM1:6 nM
体外活性	EZM2302 (GSK3359088) is an inhibitor of CARM1 enzymatic activity in biochemical assays (IC50?=?6?nM) with broad selectivity against other histone methyltransferases. Ninety-six-hour EZM2302 treatment led to a concentration-dependent decrease in methylation of PABP1 (IC50?=?0.038?μM) and SmB (increased levels of SmBme0, EC50?=?0.018?μM), as well as in multiple aDMA bands (IC50?=?0.009?μM). Similar results were also observed in the NCI-H929 and U266B1 MM cell lines.
体内活性	Tumor growth inhibition studies were performed in SCID mice bearing subcutaneous RPMI-8226 xenografts with twice daily (BID) oral dosing on four dose groups: 37.5, 75, 150 and 300?mg per kilogram (mg/kg). EZM2302 showed dose-dependent exposure and tumor growth inhibition (TGI) after 21 days in the RPMI-8226 xenograft model. Tumors in all EZM2302 dose groups measured on day 21 showed significant decreases in tumor growth compared to vehicle. Tumor growth inhibition ranged from 45% in the 37.5?mg/kg dose group to 63% in the 300?mg/kg dose group.
激酶实验	CARM1 activity was measured as previously reported for the histone methyltransferases PRMT1/6/865 and PRMT558. Briefly, CARM1 was preincubated with compounds for 30?minutes at room temperature before reactions were initiated. Final assay conditions were 0.25?nM CARM1, 30?nM 3H-S-adenosyl-methionine (SAM), and 250?nM biotinylated peptide in buffer containing 20?mM bicine, 1?mM tris(2-carboxyethyl)phosphine, 0.005% bovine skin gelatin and 0.002% Tween-20, pH 7.5. The assays were quenched by the addition of 300?μM unlabeled SAM. The quantity of 3H-labeled peptide produced was measured by Flashplate.
细胞实验	Cultured cells in linear/log phase growth were split to a seeding density of 2e5 cells/mL in 2–20mLs of media, depending on the yield required at the end of the growth period. The compound was diluted in DMSO and added to each culture vessel with a final DMSO concentration of 0.2%. Cells were allowed to grow for 96?hours. At the conclusion of each treatment period, cells were harvested by centrifugation (5?minutes, 1200?rpm), and cell pellets were rinsed once with PBS before being frozen on dry ice pending further processing.
动物实验	For the in vivo efficacy studies, there were 8 mice per dose group and each mouse was inoculated subcutaneously at the right flank. All cells were suspended in a 0.2?mL mixture of base media and Matrigel at 1:1 for tumor development. RPMI-8226 cells were inoculated at 5?×?10^6 cells/mouse and treatment began when the mean tumor sizes reached 120?mm3 (28 days post-inoculation). CB-17 SCID Mice were assigned into groups using a randomized block design. EZM2302 or vehicle (0.5% methylcellulose in water) was administered orally BID at a dose volume of 37.5, 75, 150, or 300?mg/kg for 21 days. Body weights were measured twice a week for the duration of the study. Tumor size was measured twice weekly in two dimensions using a caliper, and the volume was expressed in cubic millimeters. Animals were euthanized 3?hours post-final dose, with blood and tissues collected for analysis.

别名	GSK3359088
分子量	585.09
分子式	C29H37ClN6O5
CAS No.	1628830-21-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (170.91 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7091 mL	8.5457 mL	17.0914 mL	42.7285 mL
	5 mM	0.3418 mL	1.7091 mL	3.4183 mL	8.5457 mL
	10 mM	0.1709 mL	0.8546 mL	1.7091 mL	4.2728 mL
	20 mM	0.0855 mL	0.4273 mL	0.8546 mL	2.1364 mL
	50 mM	0.0342 mL	0.1709 mL	0.3418 mL	0.8546 mL
	100 mM	0.0171 mL	0.0855 mL	0.1709 mL	0.4273 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

EZM 2302 1628830-21-6 Chromatin/Epigenetic Histone Methyltransferase GSK 3359088 inhibit GSK3359088 Inhibitor GSK-3359088 EZM2302 EZM-2302 inhibitor

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EZM 2302

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords