Home > VEGFR & VEGFR & > Motesanib Diphosphate

Motesanib Diphosphate

二磷酸莫特塞尼,二磷酸莫替沙尼,AMG706,AMG 706,Motesanib,AMG-706,

Motesanib Diphosphate (AMG-706)是一种有效的ATP竞争性的VEGFR1/2/3抑制剂,IC50分别为2 nM/3 nM/6 nM;对Kit具有相似的抑制活性,对VEGFR选择性比PDGFR和Ret高10倍。

目录号
EY0966
EY0966
EY0966
EY0966
纯度
99.45%
99.45%
99.45%
99.45%
规格
5 mg
10 mg
25 mg
50mg
原价
952.00
1620.00
3680.00
5000.0
售价
952.00
1620.00
3680.00
5000.00
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~25 μM

  • 动物实验

    ~100 mg/kg 口服处理,每天一次或两次

  • 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] Polverino A, et al. Cancer Res, 2006, 66(17), 8715-8721.

    分子式
    C22H29N5O9P2
    分子量
    569.44
    CAS号
    857876-30-3
    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
    100 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
    NCT00427349 Gastrointestinal Carcinoid Tumor|Islet Cell Tumor|Neoplastic Syndrome Drug: AMG 706|Drug: octreotide Eastern Cooperative Oncology Group|National Cancer Institute (NCI) Phase 2 2008-09-01 2016-07-12
    NCT01836549 Anaplastic Astrocytoma|Anaplastic Ependymoma|Astrocytoma, Grade II|Ependymoma|Giant Cell Glioblastoma|Glioblastoma|Gliosarcoma|Oligodendroglioma|Brainstem Tumors Drug: imetelstat sodium Pediatric Brain Tumor Consortium|National Cancer Institute (NCI) Phase 2 2013-03-01 2016-04-08
    NCT00360867 Solid Tumors Drug: AMG 706 Amgen Phase 2 2005-12-01 2015-09-24
    NCT01731951 Primary Myelofibrosis|Secondary Myelofibrosis|Myeloid Malignancies Drug: Imetelstat Janssen Research & Development, LLC Phase 2 2012-10-01 2016-12-02
    NCT01242930 Multiple Myeloma Drug: Imetelstat (7.5 mg/kg)|Drug: lenalidomide standard of care|Drug: Imetelstat (9.4 mg/kg) Geron Corporation Phase 2 2010-11-01 2016-04-13
    NCT00574951 Fallopian Tube Cancer|Ovarian Cancer|Primary Peritoneal Cavity Cancer Drug: motesanib diphosphate Gynecologic Oncology Group|National Cancer Institute (NCI) Phase 2 2007-12-01 2015-05-29
    NCT02011126 Childhood Hepatoblastoma|Previously Treated Childhood Rhabdomyosarcoma|Recurrent Childhood Liver Cancer|Recurrent Childhood Rhabdomyosarcoma|Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Recurrent Neuroblastoma|Recurrent Osteosarcoma Drug: imetelstat sodium|Other: laboratory biomarker analysis Children's Oncology Group|National Cancer Institute (NCI) Phase 2 2014-06-01 2017-02-08
    NCT01386866 Advanced Solid Tumors Drug: AMG 706 Amgen Phase 1 2009-05-01 2011-07-14
    NCT02426086 Primary Myelofibrosis Drug: Imetelstat 9.4 milligram/kilogram (mg/kg)|Drug: Imetelstat 4.7 mg/kg Janssen Research & Development, LLC Phase 2 2015-06-01 2016-10-31
    NCT01916187 Neuroblastoma Drug: Imetelstat NCIC Clinical Trials Group|Geron Corporation|Canadian Cancer Trials Group Phase 1 2013-07-01 2014-02-07
    NCT01137968 Non-small Cell Lung Cancer Drug: imetelstat|Drug: Bevacizumab Geron Corporation Phase 2 2010-05-01 2015-12-22
    NCT02598661 Myelodysplastic Syndromes Drug: Imetelstat|Drug: Placebo Janssen Research & Development, LLC Phase 3 2015-11-01 2017-01-13
    NCT00254267 Advanced Gastrointestinal Stromal Tumor Drug: AMG 706 Amgen|Takeda Bio Development Center, Ltd Phase 2 2005-11-01 2014-02-26
    NCT02629848 Carcinoma, Non-Small-Cell Lung Drug: Motesanib|Drug: Placebo|Drug: Paclitaxel|Drug: Carboplatin Takeda Phase 3 2012-07-01 2015-12-10
    NCT00356681 Breast Neoplasms|Breast Tumors|Breast Cancer|Locally Recurrent and Metastatic Breast Cancer Drug: AMG 706 placebo|Drug: Bevacizumab|Drug: AMG 706|Drug: Paclitaxel Amgen Phase 2 2006-12-01 2015-09-24
    NCT00094835 Lung Cancer|Non-Small Cell Lung Cancer Biological: Panitumumab|Drug: Motesanib diphosphate|Drug: Paclitaxel|Drug: Carboplatin Amgen Phase 1|Phase 2 2005-01-01 2016-02-26
    NCT00369070 Advanced Non-squamous NSCLC Biological: Bevacizumab|Drug: AMG 706|Drug: Paclitaxel|Drug: Carboplatin Amgen Phase 2 2007-01-01 2016-06-09
    NCT00124189 Chronic Lymphoproliferative Diseases Drug: GRN163L Geron Corporation Phase 1 2005-07-01 2015-12-22
    NCT00093873 Tumors Drug: Anti-angiogenesis|Drug: AMG 706 Amgen Phase 1 2003-07-01 2013-05-13
    NCT01256762 Locally Recurrent or Metastatic Breast Cancer Drug: Imetelstat sodium|Drug: Bevacizumab|Drug: Paclitaxel Geron Corporation Phase 2 2010-11-01 2015-12-22

    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。

  • 相关化合物库

  • 使用AMQUAR产品发表文献后请联系我们

相关推荐

X
  • 联系人 :
  • 收件地址 :
  • 电话号码 :
  • 单位名称 :
  • 产品货号 :
  • 产品规格 :
  • 发票抬头以及单位税号 :