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首页-抗体药物偶连体和PROTACs-PROTAC-MS177
MS177

Chemical Structure : MS177

CAS No.: 2225938-86-1

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MS177 (MS-177)

货号: PC-72286Not For Human Use, Lab Use Only.

MS177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.

规格 价格 库存 数量
2 mg ￥1280 In stock
5 mg ￥1980 In stock
10 mg ￥2980 In stock
50 mg ￥4880 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MS177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.
MS177 effectively degraded cellular EZH2-PRC2, suppressed global H3K27me3 in leukaemia cells.
MS177 exhibited half-maximal degradation concentration (DC50) values of 0.2 ± 0.1 μM and 1.5 ± 0.2 μM, and maximum degradation (Dmax) values of 82% and 68%, respectively, in EOL-1 and MV4;11 cells.
MS177 efficiently suppresses EZH2-PRC2 functions, also efficiently induces Myc degradation in cancer cells, suppresses EZH2-PRC2 functions.
MS177 efficiently induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest, which is more effective than EZH2 inhibitors. MS177 (i.p. injection, 50-100 mg/kg) represses AML growth without apparent toxicity in PDX models.

物理化学性质&存储条件

分子量 914.037
分子式 C48H55N11O8
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(6-(4-(2-(3-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)propanamido)ethyl)piperazin-1-yl)pyridin-3-yl)-1-isopropyl-1H-indazole-4-carboxamide

参考文献

1. Jun Wang, et al. Nat Cell Biol. 2022 Feb 24. doi: 10.1038/s41556-022-00850-x.

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