
MS1943
CAS No. 2225938-17-8
MS1943 ( —— )
产品货号. M21747 CAS No. 2225938-17-8
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。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥2341 | 有现货 |
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10MG | ¥3872 | 有现货 |
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25MG | ¥6391 | 有现货 |
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50MG | ¥8748 | 有现货 |
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100MG | ¥11988 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称MS1943
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注意事项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
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产品简述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。
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产品描述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.
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体外实验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.
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体内实验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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同义词——
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通路Others
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靶点Other Targets
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受体——
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研究领域——
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适应症——
化学信息
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CAS Number2225938-17-8
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分子量718.93
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分子式C??H??N?O?
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纯度>98% (HPLC)
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溶解度DMSO : 125 mg/mL (173.87 mM; Need ultrasonic)
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SMILESCC(C)N(N=C1)C2=C1C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C4=CC=C(N=C4)N(CC5)CCN5CCNC(CC67C[C@H]8C[C@H](C[C@H](C8)C7)C6)=O)=C2
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Ma A, et al. Discovery of a first-in-class EZH2 selective degrader.Nat Chem Biol. 2020 Feb;16(2):214-222.
产品手册




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