Belinostat是一种新型的HDAC抑制剂,IC50为27 nM,对抵抗Cisplatin的肿瘤有效。
Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors.
0.016-10 μM
≤40 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] Plumb JA, et al. Mol Cancer Ther, 2003, 2(8), 721-728.
分子式 C15H14N2O4S |
分子量 318.35 |
CAS号 414864-00-9 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 65 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00865969 | Peripheral T-cell Lymphoma | Drug: PXD101 | Spectrum Pharmaceuticals, Inc|Onxeo | Phase 2 | 2008-12-01 | 2014-12-04 |
NCT01317927 | Solid Tumor|Hematological Malignancy | Drug: Belinostat, Warfarin | Spectrum Pharmaceuticals, Inc|Onxeo | Phase 1 | 2010-12-01 | 2015-09-21 |
NCT02679131 | Relapsed/Refractory Solid Tumors/Hematological Malignancies | Drug: Belinostat | Spectrum Pharmaceuticals, Inc | Phase 1 | 2016-03-01 | 2017-03-10 |
NCT01583777 | Advanced Cancer | Drug: Belinostat | Spectrum Pharmaceuticals, Inc | Phase 1 | 2013-09-01 | 2016-07-20 |
NCT00413075 | Solid Tumor|Lymphoma | Drug: oral belinostat | Onxeo|Spectrum Pharmaceuticals, Inc | Phase 1 | 2006-06-01 | 2015-07-07 |
NCT02142530 | Non-Hodgkin Lymphoma|Diffuse Large B-cell Lymphoma|Mantle Cell Lymphoma|Follicular Lymphoma|Peripheral T-cell Lymphoma | Drug: Carfilzomib|Drug: Belinostat | Massachusetts General Hospital|National Comprehensive Cancer Network | Phase 1 | 2014-10-01 | 2016-12-17 |
NCT00274651 | Cutaneous T-Cell Lymphoma|Peripheral T-Cell Lymphoma|Non-Hodgkin's Lymphoma | Drug: belinostat | Onxeo | Phase 2 | 2006-01-01 | 2015-07-07 |
NCT01090830 | Non-Small-Cell Lung Carcinoma | Drug: Belinostat, carboplatin, paclitaxel and bevacizumab | Holy Cross Hospital, Florida | Phase 1|Phase 2 | 2010-04-01 | 2013-03-19 |
NCT00321594 | Adult Primary Hepatocellular Carcinoma|Advanced Adult Primary Liver Cancer|Localized Unresectable Adult Primary Liver Cancer|Recurrent Adult Primary Liver Cancer | Drug: belinostat | National Cancer Institute (NCI) | Phase 1|Phase 2 | 2006-05-01 | 2013-01-30 |
NCT00421889 | Ovarian Cancer|Epithelial Ovarian Cancer|Fallopian Tube Cancer|Bladder Cancer | Drug: belinostat|Drug: Paclitaxel|Drug: Carboplatin | Onxeo | Phase 1|Phase 2 | 2005-08-01 | 2015-07-07 |
NCT02381548 | Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Previously Treated Myelodysplastic Syndrome|Recurrent Adult Acute Myeloid Leukemia|Refractory Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Secondary Acute Myeloid Leukemia|Therapy-Related Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia | Drug: Belinostat|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: WEE1 Inhibitor AZD1775 | National Cancer Institute (NCI) | Phase 1 | 2015-08-01 | 2017-02-03 |
NCT01839097 | Peripheral T-cell Lymphoma | Drug: Belinostat|Drug: CHOP | Spectrum Pharmaceuticals, Inc | Phase 1 | 2013-05-01 | 2016-04-18 |
NCT00301756 | Fallopian Tube Carcinoma|Primary Peritoneal Carcinoma|Recurrent Borderline Ovarian Surface Epithelial-Stromal Tumor|Recurrent Ovarian Carcinoma|Stage III Borderline Ovarian Surface Epithelial-Stromal Tumor|Stage III Ovarian Cancer|Stage IV Borderline Ovarian Surface Epithelial-Stromal Tumor|Stage IV Ovarian Cancer | Drug: Belinostat|Other: Laboratory Biomarker Analysis | National Cancer Institute (NCI) | Phase 2 | 2006-09-01 | 2016-10-20 |
NCT00357162 | de Novo Myelodysplastic Syndromes|Previously Treated Myelodysplastic Syndromes|Secondary Myelodysplastic Syndromes | Drug: belinostat | National Cancer Institute (NCI) | Phase 2 | 2006-05-01 | 2014-05-02 |
NCT02680795 | Solid Tumors|Hematological Malignancies | Drug: Belinostat IV|Drug: Belinostat IV|Drug: Belinostat | Spectrum Pharmaceuticals, Inc | Phase 1 | 2016-03-01 | 2017-03-10 |
NCT00334789 | Adult Solid Neoplasm | Drug: Belinostat|Drug: Isotretinoin|Other: Pharmacological Study | National Cancer Institute (NCI) | Phase 1 | 2006-06-01 | 2016-12-26 |
NCT02137759 | Glioblastoma Multiforme of Brain | Radiation: Standard Radiation Therapy|Drug: Standard Temozolomide|Drug: Belinostat | Emory University|Johns Hopkins University|Spectrum Pharmaceuticals, Inc|National Cancer Institute (NCI) | Phase 2 | 2014-05-01 | 2016-09-22 |
NCT01188707 | Non Small Cell Lung Cancer | Drug: Belinostat and Erlotinib | Herlev Hospital|Copenhagen University Hospital at Herlev|Bispebjerg Hospital|Onxeo|Roche Pharma AG | Phase 1|Phase 2 | 2010-12-01 | 2011-08-03 |
NCT01273155 | Neoplasms|Lymphomas | Drug: Belinostat | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | Phase 1 | 2010-12-22 | 2017-03-08 |
NCT01310244 | Stage IV Non-small Cell Lung Cancer | Drug: Belinostat, Carboplatin, Paclitaxel | Spectrum Pharmaceuticals, Inc|Onxeo | Phase 1|Phase 2 | 2010-12-01 | 2015-09-21 |
NCT00878800 | Dose Escalation: Solid Tumors|MTD: Soft Tissue Sarcomas | Drug: PXD101|Drug: Doxorubicin | Onxeo|Spectrum Pharmaceuticals, Inc | Phase 1|Phase 2 | 2006-12-01 | 2015-07-07 |
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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