Thioguanine是一种嘌呤类的抗代谢药物,广泛用于治疗急性淋巴细胞白血病,自身免疫性疾病(如克罗恩氏病,类风湿关节炎)和器官移植接受患者。
Thioguanine, a purine antimetabolite, inhibits DNMT1 activity through ubiquitin-targeted degradation, used in the treatment of acute lymphoblastic leukemia, autoimmune disorders (e.g., Crohn's disease, rheumatoid arthritis) and organ transplant recipients.
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] Krynetskaia NF, et al. FASEB J,2000, 14(14), 2339-2344.
分子式 C5H5N5S |
分子量 167.19 |
CAS号 154-42-7 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mM |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02141100 | Non-Hodgkin Lymphoma | Drug: 6-thioguanine | Kjeld Schmiegelow|Aalborg Universitetshospital|Aarhus University Hospital Skejby|Odense University Hospital|Rigshospitalet, Denmark | Phase 1|Phase 2 | 2014-07-01 | 2016-10-06 |
NCT00588536 | Langerhans Cell Histiocytosis | Drug: Methotrexate|Drug: 6-Thioguanine|Drug: Leucovorin Calcium | Memorial Sloan Kettering Cancer Center | Phase 2 | 1995-01-01 | 2015-04-16 |
NCT00587873 | Hodgkin's Disease | Drug: Methotrexate|Drug: Leucovorin calcium|Drug: 6-Thioguanine | Memorial Sloan Kettering Cancer Center | Phase 2 | 1994-03-01 | 2009-06-10 |
NCT02912676 | Acute Lymphoblastic Leukemia | Drug: Thioguanine (oral) | Kjeld Schmiegelow|Danish Child Cancer Foundation|Nordic Society for Pediatric Hematology and Oncology|Rigshospitalet, Denmark | Phase 1|Phase 2 | 2016-10-01 | 2016-11-03 |
NCT00504660 | Anaplastic Glioma of Brain|Glioblastoma Multiforme|Brain Cancer | Drug: Capecitabine|Drug: Celecoxib (Celebrex)|Drug: Temozolomide|Drug: Lomustine|Drug: 6-Thioguanine | M.D. Anderson Cancer Center | Phase 2 | 2003-09-01 | 2011-12-06 |
NCT00549848 | Acute Lymphoblastic Leukemia | Drug: Prednisone, Vincristine, Daunorubicin, PEG-L-asparaginase, Erwinia L-asparaginase, Doxorubicin, Cyclophosphamide, Cytarabine, Thioguanine|Drug: Clofarabine, Methotrexate, Mercaptopurine, Dexamethasone, Etoposide, Dasatinib | St. Jude Children's Research Hospital|National Cancer Institute (NCI)|Enzon Pharmaceuticals, Inc.|National Institute of General Medical Sciences (NIGMS) | Phase 3 | 2007-10-01 | 2016-08-29 |
NCT03022747 | Lymphoblastic Leukemia, Acute, Childhood | Drug: Allopurinol|Drug: Standard treatment | Vastra Gotaland Region | Phase 2 | 2017-01-01 | 2017-01-11 |
NCT00002744 | Leukemia | Drug: asparaginase|Drug: cyclophosphamide|Drug: cytarabine|Drug: daunorubicin hydrochloride|Drug: dexamethasone|Drug: doxorubicin hydrochloride|Drug: mercaptopurine|Drug: methotrexate|Drug: pegaspargase|Drug: prednisone|Drug: therapeutic hydrocortisone|Drug: thioguanine|Drug: vincristine sulfate|Radiation: low-LET cobalt-60 gamma ray therapy|Radiation: low-LET photon therapy | Children's Oncology Group|National Cancer Institute (NCI) | Phase 3 | 1996-05-01 | 2017-02-07 |
NCT00849368 | Inflammatory Bowel Disease | Drug: Azathioprine / Allopurinol | University of Zurich | Phase 1 | 2009-01-01 | 2012-02-06 |
NCT00184041 | Acute Lymphoblastic Leukemia | Drug: Daunorubicin, Vincristine, Prednisone, Methotrexate, PEG-Asparaginase, 6-Mercaptopurine, Cytoxan, Cytosine Arabinoside, VM-26 and 6-Thioguanine | University of Southern California | Phase 2 | 2004-07-01 | 2014-05-20 |
NCT00866749 | Lymphoblastic Leukemia|Lymphoblastic Lymphoma | Drug: Daunorubicin|Drug: Vincristine|Drug: PEG-asparaginase|Drug: Intrathecal Methotrexate|Drug: Cyclophosphamide|Drug: Cytarabine|Drug: Mercaptopurine|Drug: Methotrexate|Drug: Doxorubicin|Drug: Thioguanine | M.D. Anderson Cancer Center | Phase 2 | 2006-09-01 | 2016-11-07 |
NCT02598908 | External Quality Control|Thiopurine S-methyl Transferase (TPMT) | Other: Quality control - enzyme activity | Sandwell & West Birmingham Hospitals NHS Trust|Birmingham Quality | 2017-04-01 | 2016-10-19 | |
NCT00369317 | Childhood Acute Basophilic Leukemia|Childhood Acute Eosinophilic Leukemia|Childhood Acute Erythroleukemia (M6)|Childhood Acute Megakaryocytic Leukemia (M7)|Childhood Acute Minimally Differentiated Myeloid Leukemia (M0)|Childhood Acute Monoblastic Leukemia (M5a)|Childhood Acute Monocytic Leukemia (M5b)|Childhood Acute Myeloblastic Leukemia With Maturation (M2)|Childhood Acute Myeloblastic Leukemia Without Maturation (M1)|Childhood Acute Myelomonocytic Leukemia (M4)|Childhood Myelodysplastic Syndromes|de Novo Myelodysplastic Syndromes|Secondary Acute Myeloid Leukemia|Secondary Myelodysplastic Syndromes|Untreated Childhood Acute Myeloid Leukemia and Other Myeloid Malignancies | Drug: asparaginase|Drug: daunorubicin hydrochloride|Drug: cytarabine|Drug: thioguanine|Drug: etoposide|Other: laboratory biomarker analysis | Children's Oncology Group|National Cancer Institute (NCI) | Phase 3 | 2007-03-01 | 2017-02-07 |
NCT00002944 | Brain Tumors|Central Nervous System Tumors | Drug: carboplatin|Drug: lomustine|Drug: procarbazine hydrochloride|Drug: thioguanine|Drug: vincristine sulfate | Children's Oncology Group|National Cancer Institute (NCI) | Phase 3 | 1997-04-01 | 2013-09-06 |
NCT02828358 | Acute Leukemia of Ambiguous Lineage|Childhood B Acute Lymphoblastic Leukemia|Mixed Phenotype Acute Leukemia | Drug: Azacitidine|Drug: Cyclophosphamide|Drug: Cytarabine|Drug: Daunorubicin Hydrochloride|Drug: Dexamethasone|Drug: Hydrocortisone Sodium Succinate|Other: Laboratory Biomarker Analysis|Drug: Leucovorin Calcium|Drug: Mercaptopurine|Drug: Methotrexate|Drug: Pegaspargase|Other: Pharmacological Study|Drug: Prednisolone|Drug: Thioguanine|Drug: Vincristine Sulfate | National Cancer Institute (NCI) | 2016-12-01 | 2017-01-31 | |
NCT02660762 | Leukaemia,Lymphoblastic | Drug: Vincristine|Drug: Daunorubicin|Drug: Pegaspargase|Drug: Prednisone|Drug: Intrathecal Methotrexate|Drug: Cyclophosphamide|Drug: Cytarabine|Drug: 6-Mercaptopurine|Drug: Methotrexate|Drug: Etoposide|Drug: dexamethasone|Drug: thioguanine|Drug: intrathecal cytarabine | Sun Yat-sen University | Phase 2 | 2010-01-01 | 2016-10-19 |
NCT00866307 | B-cell Adult Acute Lymphoblastic Leukemia|B-cell Childhood Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia | Drug: pegaspargase|Drug: cytarabine|Drug: vincristine sulfate|Drug: doxorubicin hydrochloride|Drug: cyclophosphamide|Drug: prednisone|Drug: dexamethasone|Drug: methotrexate|Drug: daunorubicin hydrochloride|Drug: mercaptopurine|Drug: thioguanine|Radiation: prophylactic cranial irradiation|Other: laboratory biomarker analysis | Children's Oncology Group|National Cancer Institute (NCI) | 2009-02-01 | 2017-02-07 | |
NCT00003593 | Leukemia|Myelodysplastic Syndromes|Myelodysplastic/Myeloproliferative Neoplasms | Drug: asparaginase|Drug: cytarabine|Drug: daunorubicin hydrochloride|Drug: methotrexate|Drug: therapeutic hydrocortisone|Drug: thioguanine | Children's Oncology Group|National Cancer Institute (NCI) | Phase 3 | 1999-06-01 | 2013-06-26 |
NCT00109837 | Leukemia | Biological: filgrastim|Drug: cyclophosphamide|Drug: cytarabine|Drug: daunorubicin|Drug: dexamethasone|Drug: doxorubicin|Drug: leucovorin|Drug: mercaptopurine|Drug: methotrexate|Drug: mitoxantrone|Drug: Asparaginase|Drug: prednisone|Drug: thioguanine|Drug: vincristine|Radiation: radiation therapy|Drug: allopurinol|Drug: bactrim | Southwest Oncology Group|National Cancer Institute (NCI) | Phase 2 | 2005-04-01 | 2015-03-05 |
NCT01432145 | Breast Cancer|Ovarian Cancer | Drug: 6-Mercaptopurine|Drug: Methotrexate | University of Oxford | Phase 2 | 2011-05-01 | 2015-05-27 |
NCT00002816 | Leukemia | Drug: cytarabine|Drug: dexamethasone|Drug: etoposide|Drug: idarubicin|Drug: ifosfamide|Drug: leucovorin calcium|Drug: mesna|Drug: pegaspargase|Drug: therapeutic hydrocortisone|Drug: thioguanine|Drug: vincristine sulfate|Radiation: low-LET cobalt-60 gamma ray therapy|Radiation: low-LET electron therapy|Radiation: low-LET photon therapy|Drug: Methotrexate | Children's Oncology Group|National Cancer Institute (NCI) | Phase 3 | 1996-12-01 | 2013-08-21 |
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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