Cladribine (克拉屈滨) 是腺苷脱氨酶(adenosine deaminase)抑制剂,可作用于毛细胞白血病和多发性硬化。
Cladribine is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.
0 μM - 32 μM
0.7 mM - 3.5 mM腹腔注射给药
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] Ma J, et al. BMC Cancer. 2011, 11, 255.
分子式 C10H12ClN5O3 |
分子量 285.69 |
CAS号 4291-63-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO ≥55 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 |
NCT00938366 | Multiple Sclerosis | Drug: Cladribine|Drug: Pantoprazole | Merck KGaA|Merck Serono S.A., Geneva | Phase 1 | 2008-01-01 | 2016-03-15 |
NCT01013350 | Multiple Sclerosis | Drug: Cladribine | EMD Serono | 2009-11-01 | 2016-10-14 | |
NCT02115295 | Leukemia | Drug: Cladribine|Drug: Cytarabine|Drug: Idarubicin|Behavioral: Phone Calls | M.D. Anderson Cancer Center | Phase 2 | 2014-05-01 | 2016-08-10 |
NCT02131753 | Hairy Cell Leukemia | Drug: Cladribine s.c. injection, HCL treatment | University of Giessen | Phase 2|Phase 3 | 2004-05-01 | 2016-10-25 |
NCT01602939 | Systemic Mastocytosis | Drug: Cladribine and pegylated interpheron alpha-2a | Hospital Virgen de la Salud | Phase 2|Phase 3 | 2012-05-01 | 2016-08-26 |
NCT01515527 | Leukemia | Drug: Cladribine|Drug: Cytarabine|Drug: Decitabine | M.D. Anderson Cancer Center | Phase 2 | 2012-02-01 | 2017-02-14 |
NCT00002879 | Lymphoma | Drug: cladribine | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) | Phase 2 | 1996-11-01 | 2016-12-05 |
NCT00412594 | Leukemia | Drug: Cladribine|Drug: Rituximab | M.D. Anderson Cancer Center|Genentech, Inc. | Phase 2 | 2004-06-10 | 2017-01-24 |
NCT00126321 | Leukemia, Myelocytic, Acute | Drug: cladribine | University Hospital, Bonn | Phase 2 | 2004-11-01 | 2010-02-01 |
NCT00923013 | Hairy Cell Leukemia | Drug: Cladribine|Drug: Rituximab | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | Phase 2 | 2008-10-03 | 2017-02-10 |
NCT01473797 | Langerhans Cell Histiocytosis of Lung | Drug: Cladribine | Assistance Publique - Hpitaux de Paris | Phase 2 | 2011-11-01 | 2016-09-28 |
NCT00980395 | Lymphoma|Mantle Cell Lymphoma|Indolent Lymphoma|SLL | Drug: rituximab|Drug: bortezomib|Drug: cladribine | University of Arizona|National Cancer Institute (NCI) | Phase 2 | 2009-07-01 | 2016-04-13 |
NCT01446900 | Chronic Lymphocytic Leukaemia|Small Lymphocytic Lymphoma | Drug: Rituximab|Drug: Cladribine | European Institute of Oncology | Phase 2 | 2011-01-01 | 2015-09-28 |
NCT02157181 | Hairy Cell Leukemia (HCL) | Drug: 2CdA +/- Rituximab | Jurgen Barth|University of Giessen | Phase 2 | 2004-06-01 | 2014-06-03 |
NCT00053027 | Lymphoma | Biological: rituximab|Drug: cladribine | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) | Phase 2 | 2003-02-01 | 2016-12-05 |
NCT00213135 | Multiple Sclerosis, Relapsing-Remitting | Drug: Cladribine 5.25 mg/kg|Drug: Cladribine 3.5 mg/kg|Other: Placebo | EMD Serono | Phase 3 | 2005-04-01 | 2014-01-10 |
NCT01439750 | Mantle Cell Lymphoma | Drug: Rituximab|Drug: bortezomib|Drug: Cladribine | Milton S. Hershey Medical Center | Phase 1|Phase 2 | 2012-05-01 | 2017-01-26 |
NCT00725985 | Multiple Sclerosis | Drug: Cladribine|Drug: Cladribine|Drug: Placebo|Drug: Rebif new formulation (RNF) | EMD Serono | Phase 3 | 2008-12-01 | 2013-08-02 |
NCT02250937 | Acute Myeloid Leukemia|Myelodysplastic Syndrome | Drug: Busulfan|Drug: Fludarabine|Drug: Cladribine|Procedure: Stem Cell Transplant|Drug: G-CSF|Drug: Methotrexate|Drug: Cyclophosphamide | M.D. Anderson Cancer Center | Phase 2 | 2014-10-27 | 2017-03-20 |
NCT02044796 | Acute Biphenotypic Leukemia|de Novo Myelodysplastic Syndrome|Previously Treated Myelodysplastic Syndrome|Recurrent Adult Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|Secondary Myelodysplastic Syndrome|Untreated Adult Acute Myeloid Leukemia | Drug: Cladribine|Drug: Cytarabine|Biological: Filgrastim|Other: Laboratory Biomarker Analysis|Drug: Mitoxantrone Hydrochloride | Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) | Phase 1|Phase 2 | 2014-01-01 | 2016-09-26 |
NCT00436826 | Multiple Sclerosis | Drug: Cladribine|Drug: Placebo|Drug: Interferon-beta (IFN-beta) | EMD Serono | Phase 2 | 2006-11-01 | 2013-08-04 |
NCT00787969 | Lymphoma | Biological: rituximab|Drug: cladribine|Drug: temsirolimus|Biological: Filgrastim|Biological: Pegfilgrastim | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) | Phase 1 | 2009-04-01 | 2016-12-02 |
NCT00483067 | Leukemia | Drug: 2-CdA|Drug: Ara-C|Drug: G-CSF (Granulocyte colony-stimulating factor) | M.D. Anderson Cancer Center | Phase 2 | 1998-03-01 | 2012-08-01 |
NCT00667329 | Lymphoma | Drug: 2CdA|Drug: Cyclophosphamide|Drug: Rituximab | M.D. Anderson Cancer Center | 1999-07-01 | 2016-09-12 | |
NCT00656812 | Lymphoma of Mucosa-Associated Lymphoid Tissue | Drug: Rituximab|Drug: 2-CdA | Arbeitsgemeinschaft medikamentoese Tumortherapie|Hoffmann-La Roche|Lipomed | Phase 2 | 2008-05-01 | 2013-12-23 |
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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