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Panobinostat

帕比司他,LBH589,NVP-LBH589

Panobinostat (LBH589)是一种新型的,广谱的HDAC抑制剂,IC50为5 nM。

目录号
EY0821
EY0821
EY0821
EY0821
纯度
99.22%
99.22%
99.22%
99.22%
规格
5 mg
10 mg
50 mg
100 mg
原价
370
620
1650
2800
售价
370
620
1650
2800
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

    Panobinostat, as known as LBH589, is a novel and potent hydroxamic acid-based deacetylase inhibitor (DACis)that inhibits a broad spectrum of histone deacetylases (HDACs), including all Classes 1, 2 and 4 HDAC enzymes, at low nanomolar concentrations. According to previous studies, it not only induces apoptosis in multiple myeloma (MM) cells via caspase activation and poly(ADP-ribose) polymerase (PARP) cleavage, but also induces potent cell growth inhibition, cell-cycle arrest, and apoptosis in a time- and dose-dependent manner in both Philadelphia chromosome-negative (Ph-) actue lymphoblastic leukemia (ALL) cells lines (T-cell MOLT-4 and pre-B-cell Reh), which are correlated with induction of histone (H3K9 and H4K8) hyperacetylation, activation of p21 and p27, and suppression of c-Myc.

  • 体外研究

  • 体内研究

    2% DMSO, 2% Tween 80, 48% PEG 300

  • 激酶实验

  • 细胞实验

    50 nM

  • 动物实验

    10 mg/kg, 20 mg/kg 腹腔注射

  • 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] Scuto A, et al. Blood. 2008, 111(10), 5093-5100.
    [2] Catley, L., et al. 2006. Blood. 108: 3441-3449.
    [3] Fiskus, W., et al. 2006. Mol. Cancer Ther. 5: 3096-3104.
    [4] Sasaki, D., et al. 2011. Haematologica. PMID: 21228036.

    分子式
    C21H23N3O2
    分子量
    349.43
    CAS号
    404950-80-7
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    70 mg/mL
    Water
    <1 mg/mL
    Ethanol
    3 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
    NCT00931762 Primary Myelofibrosis|Post-Polycythemia Vera|Post-Essential Thrombocytopenia Drug: Panobinostat Novartis Pharmaceuticals|Novartis Phase 2 2009-07-01 2016-11-16
    NCT01245179 Sickle Cell Disease Drug: panobinostat Abdullah Kutlar|Novartis Pharmaceuticals|Augusta University Phase 1 2010-11-01 2016-06-21
    NCT01802879 Hematologic Neoplasms Drug: Panobinostat Novartis Pharmaceuticals|Novartis Phase 2 2013-06-24 2017-02-07
    NCT01496118 Multiple Myeloma Drug: carfilzomib and panobinostat SCRI Development Innovations, LLC|Onyx Therapeutics, Inc.|Novartis Phase 1|Phase 2 2011-12-01 2017-01-03
    NCT01242774 Acute Myeloid Leukemia (AML) Drug: Panobinostat Novartis Pharmaceuticals|Novartis Phase 1 2010-10-01 2015-05-05
    NCT00925132 Metastatic Melanoma Drug: Temozolomide, Decitabine, Panobinostat University of Iowa|Holden Comprehensive Cancer Center|Novartis Pharmaceuticals Phase 1|Phase 2 2009-12-01 2017-01-04
    NCT01115036 Recurrent Glioblastoma Drug: panobinostat Duke University|Novartis Phase 2 2010-04-01 2013-06-17
    NCT01451268 Myelodysplastic Syndrome|Acute Myeloid Leukemia Drug: Panobinostat|Drug: Panobinostat Johann Wolfgang Goethe University Hospital Phase 1|Phase 2 2011-01-01 2016-09-01
    NCT01680094 HIV Infection Drug: Panobinostat University of Aarhus|Massachusetts General Hospital|Monash University|University of Sydney|Novartis|Aarhus University Hospital Phase 1|Phase 2 2012-09-01 2014-02-24
    NCT01651039 Multiple Myeloma Drug: Panobinostat, Lenalidomide and Dexamethasone Ajai Chari|Novartis Pharmaceuticals|Icahn School of Medicine at Mount Sinai Phase 2 2012-07-01 2017-01-26
    NCT02717455 Glioma Drug: LBH589 Pediatric Brain Tumor Consortium Phase 1 2016-03-01 2016-11-15
    NCT01336842 Solid Tumors|Non-Small Cell Lung Cancer (NSCLC) Drug: Panobinostat, Cisplatin, Pemetrexed University of California, Davis|Novartis Pharmaceuticals Phase 1 2011-04-01 2017-01-19
    NCT00663832 Prostate Cancer Drug: LBH589 (i.v. panobinostat) Novartis Pharmaceuticals|Novartis Phase 1 2008-02-01 2012-05-15
    NCT01065467 Melanoma|Malignant Melanoma Drug: LBH589 Dana-Farber Cancer Institute|Brigham and Women's Hospital|Novartis Phase 1 2010-02-01 2017-02-15
    NCT00967044 Lymphoma Drug: Panobinostat|Drug: Everolimus M.D. Anderson Cancer Center|Novartis Phase 1|Phase 2 2009-11-01 2015-02-09
    NCT00742027 Classical Hodgkin's Lymphoma (i.e. Nodular Sclerosing, Mixed-cellularity, Lymphocyte-rich, Lymphocyte-depleted) Drug: Panobinostat Novartis Pharmaceuticals|Novartis Phase 2 2008-09-01 2016-01-16
    NCT02032810 Melanoma|Skin Cancer Drug: Panobinostat|Drug: Ipilimumab H. Lee Moffitt Cancer Center and Research Institute|Novartis Phase 1 2014-01-01 2017-03-21
    NCT00901147 Peripheral T-cell Lymphoma (Not Otherwise Specified)|Angioimmunoblastic T-cell Lymphoma|Extranodal NK/T-cell Lymphoma Nasal Type|Enteropathy- Type T-cell Lymphoma|Hepatosplenic T-cell Lymphoma|Anaplastic Large Cell Lymphoma (ALCL) (ALK-1 Negative)|Relapsed ALCL (ALK-1 Positive) Post Autologous Transplant Drug: panobinostat and bortezomib Singapore General Hospital Phase 2 2009-11-01 2014-06-26
    NCT00985946 Neuroendocrine Tumors Drug: panobinostat (LBH589) University of Wisconsin, Madison|Novartis Pharmaceuticals Phase 2 2010-05-01 2015-05-28
    NCT02899715 Diffuse Intrinsic Pontine Glioma Other: Laboratory Biomarker Analysis|Drug: Panobinostat|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2016-04-01 2016-11-01

    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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