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YM155

Sepantronium Bromide

YM155 (Sepantronium Bromide)是一种有效的survivin抑制剂，通过抑制Survivin启动子活性而发挥作用，IC50为0.54 nM；对SV40启动子活性抑制作用不显著，对Survivin与XIAP相互作用抑制效果微弱。Phase 1/2。

目录号
EY0758
EY0758
EY0758
EY0758
纯度
99.38%
99.38%
99.38%
99.38%
规格
1 mg
5 mg
10 mg
50 mg
原价
180
400
700
2200
售价
180
400
700
2200
库存
现货
现货
现货
现货
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  • 生物活性

    Sepantronium bromide, also known as YM155, is a novel small-molecule suppressant of surviving, the smallest member of inhibitor of apoptosis (IAP) gene family. It exhibits a potent suppressive activity against survivin but has little effect on expression levels of other IAP family members or B-cell lymphoma 2 (BCL-2) related proteins. YM155 also suppresses proliferation in a broad range of human cancer cell lines, induces tumor regression in non-small cell lung cancer (NSCLC), melanoma, bladder, aggressive non-Hodgkin lymphoma, and breast cancer xenograft models, reduces spontaneous metastases, and significantly prolongs the survival of animal harboring established metastatic tumors derived from a human triple-negative breast cancer (TNBC) cell lines.

  • 体外研究

  • 体内研究

    Saline

  • 激酶实验

  • 细胞实验

    1 μM

  • 动物实验

    5 mg/kg 皮下注射，每周持续处理3天，处理3周

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Nakahara T, et al. Cancer Res, 2007, 67(17), 8014-8021.

    分子式
    C20H19BrN4O3    		 分子量
    443.29    		 CAS号
    781661-94-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >89 mg/mL    		 Water
    >89 mg/mL    		 Ethanol
    >20 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01023386 Cancer Drug: YM155 Astellas Pharma Inc Phase 1 2009-11-01 2010-04-12
    NCT00818480 Prostate Cancer|Melanoma|Non-Hodgkin's Lymphoma Drug: YM155 Astellas Pharma Inc Phase 2 2006-02-01 2015-08-20
    NCT01007292 Non-Hodgkin's Lymphoma Drug: YM155|Biological: Rituximab Astellas Pharma Inc Phase 2 2009-11-01 2015-09-29
    NCT01009775 Melanoma Drug: YM155|Drug: Docetaxel Astellas Pharma Inc Phase 2 2009-11-01 2015-08-20
    NCT00498914 Lymphoma, Large-Cell, Diffuse|Lymphoma, B-Cell Refractory Drug: YM155 Astellas Pharma Inc Phase 2 2007-06-01 2015-08-20
    NCT01038804 Breast Cancer Drug: YM155|Drug: Docetaxel Astellas Pharma Inc Phase 2 2009-12-01 2013-09-12
    NCT01100931 NSCLC|Solid Tumors Drug: YM155|Drug: Carboplatin|Drug: Paclitaxel National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 1|Phase 2 2010-02-01 2015-09-29
    NCT00514267 Prostate Cancer|Tumors Drug: YM 155|Drug: Docetaxel|Drug: Prednisone Astellas Pharma Inc Phase 1|Phase 2 2007-05-01 2015-07-23
    NCT00281541 Melanoma Drug: YM155 Astellas Pharma Inc|Astellas Pharma US, Inc. Phase 2 2005-11-01 2012-06-06
    NCT00328588 Lung Cancer|Cancer of Lung|Cancer of the Lung|Non-Small Cell Lung Carcinoma|Carcinoma, Non-Small Cell Lung Drug: YM155 Astellas Pharma Inc Phase 2 2006-12-01 2007-12-26
    NCT00257478 Prostate Cancer|Cancer of Prostate|Prostatic Cancer|Cancer of the Prostate Drug: YM155 Astellas Pharma Inc|Astellas Pharma US, Inc. Phase 2 null 2012-06-06

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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