MS1943

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MS1943 是一流的、口服生物可利用的 EZH2 选择性降解剂，IC50 为 120 nM。 MS1943 显着降低多种三阴性乳腺癌 (TNBC) 以及其他癌症和非癌细胞系中的 EZH2 蛋白水平。

MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines.

MS1943 (0.625-5 μM; 3 days) inhibits cell growth with an GI50 of 2.2 μM.MS1943 (0.625-5 μM; 4 days) 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.MS1943 (1.25-5.0 μM; 2 days) inhibits EZH2 and SUZ12 protein levels in a concentration- and timedependent manner, without affecting EED protein levels, whereas the H3K27me3 mark was also suppressed. Cell Viability Assay Cell Line:MDA-MB-468 cells Concentration:0.625, 1.25, 2.5, 5 μM Incubation Time:3 days Result:Inhibits cell growth with an GI50 of 2.2 μM.Western Blot Analysis Cell Line:MDA-MB-468 cells Concentration:1.25, 2.5, 5.0 μM Incubation Time:2 daysResult:Reduced EZH2 protein levels in a concentration- and time-dependent manner.

MS1943 (150 mg/kg body weight; i.p.; once daily for 36 days) suppresses tumor growth.MS1943 induces apoptosis in the MDA-MB-468 xenograft model.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. Animal Model:Eight-week-old female BALB/c nude mice (MDA-MB-468 xenografts) Dosage:150 mg/kg body weight Administration:i.p.; once daily for 36 days Result:Suppresses tumor growth.

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2225938-17-8

718.93

C??H??N?O?

>98% (HPLC)

DMSO : 125 mg/mL (173.87 mM; Need ultrasonic)

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(-20℃)

With Ice Pack

≥ 2 years