• 咨询热线
    客服服务热线 13671568941/15317326293
  • 在线咨询
  • 微信客服
    微信客服
  • 公众号
    扫码关注公众号

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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥2341 有现货
10MG ¥3872 有现货
25MG ¥6391 有现货
50MG ¥8748 有现货
100MG ¥11988 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    MS1943
  • 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
  • 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。
  • 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.
  • 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.
  • 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.
  • 同义词
    ——
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    ——
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    2225938-17-8
  • 分子量
    718.93
  • 分子式
    C??H??N?O?
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO : 125 mg/mL (173.87 mM; Need ultrasonic)
  • SMILES
    CC(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
  • 化学全称
    ——

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 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
关联产品
  • Amosulalol

    阿莫洛尔是一种肾上腺素能化合物。

  • Ganoderenic acid H

    Ganoderenic acid H is one compound of triterpenoids isolated from Ganoderma lucidum, triterpenoids exhibit a broad spectrum of anti-cancer properties, including anti-proliferative, anti-metastatic and anti-angiogenic activities.

  • 1,3,5-tris(pyridin-4...

    1,3,5-三(吡啶-4-基乙炔基)苯是一种化合物。