LDE225

Sonidegib,NVP-LDE225,Erismodegib

LDE225 (NVP-LDE225,Erismodegib)是一种Smoothened(Smo)拮抗剂,抑制Hedgehog (Hh)信号通路,IC50分别为1.3 nM (小鼠)和2.5 nM(人)。

目录号
EY1212
EY1212
EY1212
纯度
99.54%
99.54%
99.54%
规格
5 mg
10 mg
50 mg
原价
610
880
2750
售价
610
880
2750
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    LDE225(synonym: LDE-225, NVP-LDE225, Erismodegib) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.

  • 体外研究

  • 体内研究

    0.5% CMC

  • 激酶实验

  • 细胞实验

    0 μM -10 μM

  • 动物实验

    40 mg/kg/天口服,每天两次

  • 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] Pan SF, et al. ACS Med. Chem. Lett., 2010, 1 (3), 130–134.

    分子式
    C26H26F3N3O3
    分子量
    485.5
    CAS号
    956697-53-3
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    >90 mg/mL
    Water
    <1 mg/mL
    Ethanol
    >90 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
    NCT02111187 Prostate Cancer Drug: LDE225 Sidney Kimmel Comprehensive Cancer Center Phase 1 2014-04-01 2016-10-14
    NCT02195973 Recurrent Ovarian Cancer Drug: LDE225 University of Alabama at Birmingham|Novartis Pharmaceuticals Phase 1 2014-09-01 2017-02-06
    NCT01764776 Normal Hepatic Function|Impaired Hepatic Function Drug: LDE225 Novartis Pharmaceuticals|Novartis Phase 1 2013-03-01 2017-02-13
    NCT02086513 Graft Versus Host Disease Drug: LDE225 Massachusetts General Hospital|Novartis Phase 1 2014-04-01 2017-03-21
    NCT02254551 Multiple Myeloma Drug: LDE225|Drug: Bortezomib SCRI Development Innovations, LLC|Novartis Phase 2 2015-01-01 2016-12-23
    NCT01529450 Basal Cell Carcinoma Drug: LDE225 Anne Chang|Novartis|Stanford University 2012-02-01 2016-11-23
    NCT02002689 PTCH1 or SMO Activated Solid and Hematologic Tumors Drug: LDE225 Novartis Pharmaceuticals|Novartis Phase 2 2014-02-01 2016-04-25
    NCT01954355 Solid Tumor|Ovarian Cancer Drug: LDE225|Drug: Paclitaxel Swiss Group for Clinical Cancer Research Phase 1 2013-09-01 2016-11-23
    NCT01208831 Advanced Solid Tumor Cancers|Medulloblastoma|Basal Cell Carcinoma Drug: LDE225 Novartis Pharmaceuticals|Novartis Phase 1 2010-10-01 2016-04-20
    NCT00880308 Advanced Solid Tumor Cancers|Medulloblastoma|Basal Cell Carcinoma Drug: LDE225 Novartis Pharmaceuticals|Novartis Phase 1 2009-03-01 2014-12-27
    NCT02151864 Hepatocellular Carcinoma|Cirrhosis Drug: LDE225 Jason K. Sicklick, M.D.|Novartis Pharmaceuticals|University of California, San Diego Phase 1 2014-07-01 2016-09-27
    NCT01487785 Pancreatic Cancer Drug: LDE225+gemcitabine Novartis Pharmaceuticals|Novartis Phase 1 2012-03-01 2016-01-24
    NCT01826214 Acute Leukemias Drug: LDE225 Novartis Pharmaceuticals|Novartis Phase 2 2013-05-01 2016-07-26
    NCT02027376 Advanced Breast Cancer Drug: LDE225|Drug: Docetaxel Spanish Breast Cancer Research Group|Novartis Phase 1 2014-05-01 2015-11-05
    NCT01125800 Medulloblastoma|Rhabdomyosarcoma|Neuroblastoma|Hepatoblastoma|Glioma|Astrocytoma Drug: LDE225 Novartis Pharmaceuticals|Novartis Phase 1|Phase 2 2011-02-01 2017-02-13
    NCT01579929 Lung Cancer Drug: LDE225, Etoposide and Cisplatin Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals Phase 1 2012-04-01 2017-02-15
    NCT01694589 Resectable Pancreatic Cancer Drug: LDE-225 Rutgers, The State University of New Jersey|Rutgers Cancer Institute of New Jersey|National Cancer Institute (NCI)|Novartis Pharmaceuticals Early Phase 1 2012-11-01 2014-12-10
    NCT02138929 Esophageal Cancer Drug: Everolimus|Drug: LDE 225 M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI) Phase 1 2014-11-01 2016-09-30
    NCT01456676 Philadelphia Chromosome Positive Chronic Myelogenous Leukemia Drug: Nilotinib + LDE225 Novartis Pharmaceuticals|Novartis Phase 1 2012-01-01 2016-09-01
    NCT01327053 Basal Cell Carcinoma Drug: LDE225 Novartis Pharmaceuticals|Novartis Phase 2 2011-06-01 2016-09-20

    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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