MS1943 是一种具有口服生物活性的EZH2选择性降解剂，IC50为 120 nM。它显著降低了许多三阴性乳腺癌和其他癌及非癌细胞系中的EZH2蛋白水平，能有效阻止多个三阴性乳腺癌和其他癌细胞系的增殖。

MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).

MS1943 inhibits cell growth (GI50 of 2.2 μM). MS1943 induces cell death in MDA-MB-468 cells. MS1943 effectively reduces EZH2 levels in BT549, HCC70 and MDA-MB-231 TNBC cells, as well as KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells[1].

A single i.p. injection of MS1943 at 50 mg/kg body weight achieved a peak plasma concentration (Cmax) of 2.9 μM and resulted in plasma concentrations above its cellular IC50 value for ~2h. A single 150 mg/kg body weight p.o. dose achieved Cmax of 1.1 μM, but plasma concentrations were below the cellular IC50 value.MS1943 suppresses tumor growth[1].

2225938-17-8

C42H54N8O3

718.93

DMSO:120mg/mL (166.91mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years