Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: < 1mg/ml (insoluble)
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
EZM 2302 1628830-21-6 Chromatin/Epigenetic Histone Methyltransferase GSK 3359088 inhibit GSK3359088 Inhibitor GSK-3359088 EZM2302 EZM-2302 inhibitor