MS177 是一种有效且快速起效的 EZH2 降解剂。MS177 是一种 PROTAC 分子，由 CRBN 配体、连接子和有效的酶促 EZH2 抑制剂 C24 组成 (C24 IC₅₀: 12 nM)。MS177 可有效地消耗剥离 EZH2-PRC2 和非经典 EZH2-cMyc 复合物。MS177 抑制白血病细胞生长、诱导细胞凋亡和细胞周期阻滞。

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 IC 50 ): 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.

Solid

EZH2

MS177 inhibits the enzymatic activities of EZH2-PRC2 (IC50: 7?nM).
MS177 (5 μM, 24 h) decreases H3K27me3 and increases H3K27activity in HeLa cells.
MS177 (0.1-5 μM, 16 h) effectively degrades cellular EZH2-PRC2 and suppresses global H3K27me3 in EOL-1 cells.
MS177 (0.1-5 μM, 16 h) induces Myc degradation in EOL-1 and MV4 cells.
MS177 (4 days) shows antiproliferation effects in a panel of MLL-r leukaemia cells and samples from patients with AML, with IC50s below 2 μM.
MS177 (0.5-2.5 μM, 24 h) decreases colony-forming capabilities in MV4;11 cells.
MS177 (0.5-2.5 μM, 24 h) slows cell cycle progression and induces MOLM-13 cell apoptosis.
has not independently confirmed the accuracy of these methods. They are for reference only.

MS177 (100?mg/kg, i.p., BID for 6 days) represses tumor growth in PDX animal model of MLL-r AML, and in subcutaneously xenografted MLL-r leukaemia models.
MS177 (50 mg/kg, i.p.) achieves intraplasma concentrations about 1 μM in male Swiss Albino mice.
MS177 (100?mg/kg, i.p., BID for 6?days per week; and 200?mg/?kg, i.p. BID 3?days per week) is well tolerated and lacks apparent toxicity in mice.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

In Vitro: DMSO : 125 mg/mL (136.76 mM; Need ultrasonic)配制储备液