Cytarabine (阿糖胞苷; AraC)具有抗代谢和抗DNA合成活性。
Cytarabine (Cytosine arabinoside, AraC) is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM. Nucleoside analog of deoxycytidine; inhibits DNA replication by incorporating into DNA (IC50 = 0.04 μM in L1210 and CEM cell lines). Displays no inhibitory effects on RNA synthesis. Causes S phase cell cycle arrest in ML-1 cell lines; cytotoxic in L5817Y leukemia cells. Alternate studies suggest that 1-β-D-Arabinofuranosylcytosine is clastogenic to both spermatogonial cells and bone marrow. Furthermore, 1-β-D-Arabinofuranosylcytosine can be used to control the proliferation of glial cells.
Saline
100 μM 左右
5-1000 mg/kg静脉注射
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] Tobias SC, et al. Mol Pharm, 2004, 1(2), 112-116.
[2] Furth, J.J. and Cohen, S.S. 1968. Cancer Res. 28: 2061-2067.
[3] Kligerman, A.D., et al. 1999. Mutat. Res. 444: 151-158.
[4] Palo, A.K., et al. 2009. Mutat. Res. 673: 29-36.
分子式 C9H13N3O5 |
分子量 243.22 |
CAS号 147-94-4 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 1 mg/mL |
Water 50 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01191541 | Leukemia | Drug: Ara-c | Chinese Academy of Medical Sciences | 2010-05-01 | 2010-08-30 | |
NCT00334074 | Acute Myelogenous Leukemia|Myelodysplastic Syndromes|Chronic Myelogenous Leukemia | Drug: Clofarabine and Cytarabine | Baylor Research Institute | Phase 2 | 2005-08-01 | 2013-07-15 |
NCT02652871 | Leukemia | Drug: LY2510924|Drug: Idarubicin|Drug: Cytarabine | M.D. Anderson Cancer Center|Eli Lilly and Company|High Impact Clinical Research Support Program | Phase 1 | 2016-05-01 | 2017-01-05 |
NCT00541866 | Acute Myeloid Leukemia | Drug: voreloxin injection and cytarabine | Sunesis Pharmaceuticals | Phase 1|Phase 2 | 2007-08-01 | 2012-06-05 |
NCT02649764 | Leukemia | Drug: Fludarabine|Drug: Cytarabine|Drug: LY2606368 | M.D. Anderson Cancer Center|Eli Lilly and Company | Phase 1 | 2016-05-01 | 2017-02-16 |
NCT01034410 | Acute Myeloid Leukemia | Drug: AS1411|Drug: Cytarabine | Antisoma Research | Phase 2 | 2010-01-01 | 2011-02-01 |
NCT02718755 | Hematologic Malignancy | Drug: Fludarabine|Drug: Cytarabine|Drug: Erwinase | M.D. Anderson Cancer Center|Jazz Pharmaceuticals | Phase 2 | 2016-12-01 | 2016-09-19 |
NCT01892371 | Leukemia | Drug: Quizartinib|Drug: Cytarabine|Drug: AZA | M.D. Anderson Cancer Center|Ambit Biosciences Corporation|Celgene|National Cancer Institute (NCI) | Phase 1|Phase 2 | 2013-11-01 | 2017-03-09 |
NCT00513305 | Acute Myeloid Leukemia | Drug: Arsenic trioxide|Drug: Low-dose cytarabine alone | Cephalon|Teva Pharmaceutical Industries | Phase 3 | 2007-10-01 | 2012-07-24 |
NCT02926586 | Acute Myeloid Leukemia|Core-Binding Factor | Drug: Fludarabine|Drug: Cytarabine | Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine | Phase 4 | 2016-07-01 | 2016-10-05 |
NCT02840539 | Mantle Cell Lymphoma | Drug: Bortezomib, Cytarabine, Dexamethasone, Pegteograstim | Seoul National University Hospital|Consortium for Improving Survival of Lymphoma | Phase 2 | 2016-10-01 | 2016-11-01 |
NCT00780143 | Relapsed/Refractory Leukemia | Drug: Plitidepsin plus Cytarabine | PharmaMar | Phase 1|Phase 2 | 2007-11-01 | 2014-10-27 |
NCT02930109 | Acute Leukemia | Drug: PTX-200|Drug: Cytarabine | Prescient Therapeutics, Ltd. | Phase 1|Phase 2 | 2016-09-01 | 2016-10-07 |
NCT01615757 | Acute Myeloid Leukemia | Drug: Ara-c|Drug: Ara-c | All India Institute of Medical Sciences, New Delhi | Phase 3 | 2012-08-01 | 2012-09-13 |
NCT01960387 | Acute Myeloid Leukemia | Drug: Clofarabine|Drug: Cytarabine | University of Pittsburgh | Phase 2 | 2013-10-01 | 2016-06-21 |
NCT03021330 | AML | Drug: Daunomycin and Cytarabine (DA Regimen)|Drug: Daunomycin and Cytarabine (Intermediate Dose of DA Regimen) | Institute of Hematology & Blood Diseases Hospital | Phase 3 | 2017-02-08 | 2017-02-28 |
NCT00004263 | Leukemia|Myelodysplastic Syndromes | Drug: 7-hydroxystaurosporine (UCN-01)|Drug: Cytarabine (Ara-C) | M.D. Anderson Cancer Center|National Cancer Institute (NCI) | Phase 1 | 1999-12-01 | 2012-07-27 |
NCT00422591 | Leukemia|Acute Myeloid Leukemia|AML | Drug: Cytarabine|Drug: Idarubicin | M.D. Anderson Cancer Center | Phase 2 | 2006-12-01 | 2017-01-17 |
NCT01656031 | Leukemia | Drug: clofarabine|Drug: cytarabine | Wake Forest University Health Sciences|National Cancer Institute (NCI) | Phase 2 | 2005-02-01 | 2017-02-20 |
NCT00516828 | Leukemia|Myelodysplastic Syndromes | Drug: cytarabine | NCIC Clinical Trials Group|Canadian Cancer Trials Group | Phase 1|Phase 2 | 2007-07-01 | 2015-10-05 |
NCT01191801 | Leukemia|Acute Myeloid Leukemia|Acute Nonlymphocytic Leukemia | Drug: vosaroxin and cytarabine|Drug: placebo and cytarabine | Sunesis Pharmaceuticals | Phase 3 | 2010-10-01 | 2013-10-10 |
NCT02670707 | Langerhans Cell Histiocytosis | Drug: Cytarabine|Drug: Vinblastine/prednisone | Baylor College of Medicine|Texas Children's Hospital | Phase 3 | 2016-03-01 | 2017-01-21 |
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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