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MAK683 hydrochloride胚胎外胚层发育 (EED) 抑制剂,也是一种高效的 PRC2 抑制剂,可阻断癌细胞增殖(IC50=1.014),在EED Alphascreen, ELISA 和 LC-MS 试验中测得的IC50 值分别为 59,26,89 nM。
MAK683 hydrochloride胚胎外胚层发育 (EED) 抑制剂,也是一种高效的 PRC2 抑制剂,可阻断癌细胞增殖(IC50=1.014),在EED Alphascreen, ELISA 和 LC-MS 试验中测得的IC50 值分别为 59,26,89 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,300 | 现货 | |
5 mg | ¥ 2,920 | 现货 | |
10 mg | ¥ 4,380 | 现货 | |
25 mg | ¥ 7,220 | 现货 | |
50 mg | ¥ 9,730 | 现货 | |
100 mg | ¥ 13,100 | 现货 |
产品描述 | MAK683 hydrochloride embryonic ectodermal development (EED) inhibitor, also a potent PRC2 inhibitor, blocked cancer cell proliferation (IC50=1.014nM), with IC50 values of 59, 26, and 89 nM measured in EED Alphascreen, ELISA, and LC-MS assays, respectively. |
体外活性 | 方法:人类宫颈癌HeLa细胞使用MAK683(1.5-370nM)处理72小时,WesternBlot实验观察H3K27me3蛋白表达。 结果:MAK683 剂量依赖性地抑制 HeLa 中H3K27me3蛋白表达,IC50 约为 1.014nM。[1] |
体内活性 | 方法:为检测体内抗肿瘤活性,WT G401 或 p16 敲除细胞洗涤并重悬于冷 PBS 中之后将肿瘤细胞混合物皮下注射到雌性Balb / c裸鼠中,当肿瘤体积达到60-350毫米左右时,对小鼠进行编号并随机分配到100 mg/kg MAK683治疗组,早上8点给药,每3天测量并记录小鼠体重和肿瘤体积。 结果:MAK683治疗显著抑制抑制雌性小鼠G401 WT或p16 KO细胞的增殖[1] |
分子量 | 412.85 |
分子式 | C20H18ClFN6O |
CAS No. | 2170606-94-5 |
Smiles | FC1=CC=C2C(CCO2)=C1CNC3=NC=C(C(C=CC=N4)=C4C)C5=NN=CN35.Cl |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 4.55 mg/mL (11.01 mM) 10% DMSO+90% Saline: 0.46 mg/mL (1.11 mM), In vivo: Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
10% DMSO+90% Saline/DMSO
DMSO
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