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Birinapant

TL32711,TL 32711,TL-32711

Birinapant为二价Smac类似物,是XIAP和cIAP1的拮抗剂,Kd分别为45 nM和<1 nM。

目录号
EY0759
EY0759
EY0759
纯度
98.75%
98.75%
98.75%
规格
1 mg
2 mg
10 mg
原价
500
700
1880
售价
500
700
1880
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Birinapant (formerly TL32711) is a Smac mimetic acts as antagonist to cIAP1 and cIAP2.

  • 体外研究

  • 体内研究

    15% Captisol

  • 激酶实验

  • 细胞实验

    1 nM-1 μM

  • 动物实验

    30 mg/kg 每周腹腔注射3次

  • 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 AKm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] Allensworth JL, et al. Breast Cancer Res Treat, 2013, 137(2), 359-371.

    分子式
    C42H56F2N8O6
    分子量
    806.94
    CAS号
    1260251-31-7
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    100 mg/mL
    Water
    <1 mg/mL
    Ethanol
    50 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
    NCT02587962 Solid Tumors Drug: Birinapant|Drug: Pembrolizumab TetraLogic Pharmaceuticals|Merck Sharp & Dohme Corp. Phase 1|Phase 2 2017-02-01 2016-10-18
    NCT02147873 Myelodysplastic Syndrome (MDS)|Chronic Myelomonocytic Leukemia (CMML) Drug: birinapant|Drug: Azacitidine|Drug: Placebo TetraLogic Pharmaceuticals Phase 2 2014-06-01 2016-10-18
    NCT01940172 Relapsed Epithelial Ovarian Cancer|Relapsed Primary Peritoneal Cancer|Relapsed Fallopian Tube Cancer Drug: Birinapant|Drug: Conatumumab TetraLogic Pharmaceuticals Phase 1 2013-11-01 2016-01-13
    NCT01828346 Myelodysplastic Syndrome Drug: Birinapant|Drug: 5-Azacitidine TetraLogic Pharmaceuticals Phase 1|Phase 2 2013-06-01 2016-04-19
    NCT01188499 Cancer Drug: Birinapant TetraLogic Pharmaceuticals Phase 1|Phase 2 2010-10-01 2016-04-21
    NCT02288208 Hepatitis B Drug: Antiviral Therapy (tenofovir or entecavir)|Drug: Birinapant|Drug: Placebo (for birinapant) TetraLogic Pharmaceuticals Phase 1 2014-11-01 2016-02-04
    NCT02756130 Advanced Newly Diagnosed or Recurrent High Grade Serous Carcinomas (HGSC) Drug: Birinapant|Drug: Paclitaxel|Drug: Carboplatin Jonsson Comprehensive Cancer Center|TetraLogic Pharmaceuticals Phase 2 2017-01-01 2017-01-20
    NCT01681368 Epithelial Ovarian Cancer|Peritoneal Neoplasms|Fallopian Tube Neoplasms Drug: Birinapant (TL32711) National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 2 2012-08-01 2015-10-14
    NCT00993239 Cancer Drug: Birinapant (TL32711) TetraLogic Pharmaceuticals Phase 1 2009-11-01 2016-03-01
    NCT01573780 Unspecified Adult Solid Tumor, Protocol Specific Drug: Smac mimetic TL32711|Drug: gemcitabine hydrochloride|Other: laboratory biomarker analysis|Other: pharmacological study|Procedure: biopsy Roswell Park Cancer Institute|National Cancer Institute (NCI)|TetraLogic Pharmaceuticals Phase 1 2012-04-01 2014-01-14
    NCT01766622 Ovarian Neoplasms|Ovarian Cancer|Fallopian Tube Neoplasms|Fallopian Tube Cancer Drug: [18F]-CP18|Procedure: PET/ CT National Institutes of Health Clinical Center (CC)|National Cancer Institute (NCI) Phase 2 2012-11-30 2017-01-24
    NCT01486784 Acute Myelogenous Leukemia Drug: TL32711 Abramson Cancer Center of the University of Pennsylvania Phase 1|Phase 2 2011-11-01 2017-01-24

    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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