MS1943 是一种首创的，具有口服生物活性的 EZH2 选择性降解剂，其IC₅₀ 为 120 nM。MS1943 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。MS1943 有效地阻止了多个三阴性乳腺癌和其他癌细胞系的增殖。

MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC 50 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.

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EZH2 120 nM (IC50)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC 50 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 IC 50 value. 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

[1]. Ma A, et al. Discovery of a first-in-class EZH2 selective degrader.Nat Chem Biol. 2020 Feb;16(2):214-222.

In Vitro: DMSO : 125 mg/mL (173.87 mM; Need ultrasonic)配制储备液