2225938-86-1
中文名稱
化合物 MS-177
英文名稱
1H-Indazole-4-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[6-[4-[2-[[3-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]-1-oxopropyl]amino]ethyl]-1-piperazinyl]-3-pyridinyl]-1-(1-methylethyl)-
CAS
2225938-86-1
分子式
C48H55N11O8
分子量
914.02
MOL 文件
2225938-86-1.mol
2225938-86-1 結構式
基本信息
中文別名
化合物 MS-177 英文別名
MS1771H-Indazole-4-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[6-[4-[2-[[3-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]-1-oxopropyl]amino]ethyl]-1-piperazinyl]-3-pyridinyl]-1-(1-methylethyl)-
所屬類別
醫(yī)藥中間體：原料藥中間體物理化學性質
沸點1203.6±65.0 °C(Predicted)
密度1.44±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 2mg/mL, clear (Warmed)
酸度系數(shù)(pKa)10.74±0.40(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
應用領域
用途一
MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12?nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest.