Panobinostat (LBH589)是一种新型的,广谱的HDAC抑制剂,IC50为5 nM。
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.
2% DMSO, 2% Tween 80, 48% PEG 300
50 nM
10 mg/kg, 20 mg/kg 腹腔注射
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。
[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
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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