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Triapine

3-AP

Triapine 是一种有效的ribonucleotide reductase 抑制剂，通过抑制DNA的合成而具有广谱抗肿瘤活性。

目录号
EY1590
EY1590
纯度
99.45%
99.45%
规格
1 mg
5 mg
原价
680
1360
售价
680
1360
库存
现货
现货
订购
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  • 生物活性

    Triapine is a potent ribonucleotide reductase inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~10 μM

  • 动物实验

    ~24mg/kg 腹腔注射或静脉注射

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    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。

  • 参考文献

    [1] Finch RA, et al. Biochem Pharmacol. 2000, 59(8), 983-991.

    分子式
    C7H9N5S    		 分子量
    195.24    		 CAS号
    200933-27-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    20 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00075504 Stage II Gallbladder Cancer|Stage IIIA Gallbladder Cancer|Stage IIIB Gallbladder Cancer|Stage IVA Gallbladder Cancer|Stage IVB Gallbladder Cancer Drug: triapine|Drug: gemcitabine National Cancer Institute (NCI) Phase 2 2003-11-01 2015-08-31
    NCT00390052 Unspecified Adult Solid Tumor, Protocol Specific Drug: triapine|Other: pharmacological study|Procedure: laboratory biomarker analysis National Cancer Institute (NCI) Phase 1 2006-12-01 2013-12-13
    NCT00288093 Pancreatic Adenocarcinoma|Stage III Pancreatic Cancer Radiation: 3-Dimensional Conformal Radiation Therapy|Drug: Triapine National Cancer Institute (NCI) Phase 1 2006-12-01 2017-01-31
    NCT00085371 Acinar Cell Adenocarcinoma of the Pancreas|Duct Cell Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer Drug: triapine National Cancer Institute (NCI) Phase 2 2004-07-01 2013-10-07
    NCT00077350 Recurrent Non-small Cell Lung Cancer Drug: triapine|Drug: gemcitabine hydrochloride|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2004-07-01 2013-02-26
    NCT00293345 Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Primary Central Nervous System Hodgkin Lymphoma|Primary Central Nervous System Non-Hodgkin Lymphoma|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Stage III Adult Burkitt Lymphoma|Stage III Adult Diffuse Large Cell Lymphoma|Stage III Adult Diffuse Mixed Cell Lymphoma|Stage III Adult Diffuse Small Cleaved Cell Lymphoma|Stage III Adult Hodgkin Lymphoma|Stage III Adult Immunoblastic Large Cell Lymphoma|Stage III Adult Lymphoblastic Lymphoma|Stage III Adult T-cell Leukemia/Lymphoma|Stage III Cutaneous T-cell Non-Hodgkin Lymphoma|Stage III Grade 1 Follicular Lymphoma|Stage III Grade 2 Follicular Lymphoma|Stage III Grade 3 Follicular Lymphoma|Stage III Mantle Cell Lymphoma|Stage III Marginal Zone Lymphoma|Stage III Mycosis Fungoides/Sezary Syndrome|Stage III Small Lymphocytic Lymphoma|Stage IV Adult Burkitt Lymphoma|Stage IV Adult Diffuse Large Cell Lymphoma|Stage IV Adult Diffuse Mixed Cell Lymphoma|Stage IV Adult Diffuse Small Cleaved Cell Lymphoma|Stage IV Adult Hodgkin Lymphoma|Stage IV Adult Immunoblastic Large Cell Lymphoma|Stage IV Adult Lymphoblastic Lymphoma|Stage IV Adult T-cell Leukemia/Lymphoma|Stage IV Cutaneous T-cell Non-Hodgkin Lymphoma|Stage IV Grade 1 Follicular Lymphoma|Stage IV Grade 2 Follicular Lymphoma|Stage IV Grade 3 Follicular Lymphoma|Stage IV Mantle Cell Lymphoma|Stage IV Marginal Zone Lymphoma|Stage IV Mycosis Fungoides/Sezary Syndrome|Stage IV Small Lymphocytic Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific|Waldenstrm Macroglobulinemia Drug: gemcitabine hydrochloride|Drug: triapine National Cancer Institute (NCI) Phase 1 2006-06-01 2013-09-27
    NCT00335998 Recurrent Cervical Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Vaginal Cancer|Recurrent Vulvar Cancer|Stage III Vaginal Cancer|Stage IIIA Cervical Cancer|Stage IIIA Ovarian Epithelial Cancer|Stage IIIA Vulvar Cancer|Stage IIIB Cervical Cancer|Stage IIIB Ovarian Epithelial Cancer|Stage IIIB Vulvar Cancer|Stage IIIC Ovarian Epithelial Cancer|Stage IIIC Vulvar Cancer|Stage IV Ovarian Epithelial Cancer|Stage IVA Cervical Cancer|Stage IVA Vaginal Cancer|Stage IVB Cervical Cancer|Stage IVB Vaginal Cancer Drug: triapine|Other: laboratory biomarker analysis|Radiation: external beam radiation therapy|Radiation: brachytherapy|Drug: cisplatin|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2006-03-01 2013-01-10
    NCT00077181 Accelerated Phase Chronic Myelogenous Leukemia|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Blastic Phase Chronic Myelogenous Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia Drug: cytarabine|Drug: triapine|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 1 2004-01-01 2013-01-23
    NCT00077545 Adenocarcinoma of the Esophagus|Recurrent Esophageal Cancer|Stage IV Esophageal Cancer Drug: triapine|Drug: cisplatin National Cancer Institute (NCI) Phase 2 2004-01-01 2013-10-07
    NCT00095888 Male Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer Drug: triapine|Drug: gemcitabine hydrochloride|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 2 2004-10-01 2013-01-15
    NCT00081276 Primary Peritoneal Cavity Cancer|Recurrent Ovarian Epithelial Cancer|Stage III Ovarian Epithelial Cancer|Stage IV Ovarian Epithelial Cancer Drug: triapine|Drug: cisplatin|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2005-07-01 2013-01-23
    NCT02595879 Cervical Adenocarcinoma|Cervical Adenosquamous Carcinoma|Cervical Squamous Cell Carcinoma, Not Otherwise Specified|Stage IB Vulvar Cancer|Stage IB2 Cervical Cancer|Stage II Vulvar Cancer|Stage IIA1 Cervical Cancer|Stage IIA2 Cervical Cancer|Stage IIB Cervical Cancer|Stage IIIA Cervical Cancer|Stage IIIA Vulvar Cancer|Stage IIIB Cervical Cancer|Stage IIIB Vulvar Cancer|Stage IIIC Vulvar Cancer|Stage IVA Cervical Cancer|Stage IVA Vulvar Cancer|Vulvar Adenocarcinoma|Vulvar Squamous Cell Carcinoma Drug: Cisplatin|Radiation: External Beam Radiation Therapy|Radiation: High-Dose Rate Brachytherapy|Radiation: Intensity-Modulated Radiation Therapy|Radiation: Internal Radiation Therapy|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Triapine National Cancer Institute (NCI) Phase 1 2016-05-01 2017-01-31
    NCT00079014 Unspecified Adult Solid Tumor, Protocol Specific Drug: triapine|Drug: doxorubicin hydrochloride|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2004-01-01 2013-05-15
    NCT00084877 Unspecified Adult Solid Tumor, Protocol Specific Drug: triapine|Drug: irinotecan hydrochloride|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2004-03-01 2013-05-15
    NCT00941070 Recurrent Cervical Cancer|Recurrent Vaginal Cancer|Stage IB Cervical Cancer|Stage II Vaginal Cancer|Stage IIA Cervical Cancer|Stage IIB Cervical Cancer|Stage III Cervical Cancer|Stage III Vaginal Cancer|Stage IVA Cervical Cancer|Stage IVA Vaginal Cancer|Stage IVB Cervical Cancer|Stage IVB Vaginal Cancer|Therapy-related Toxicity Drug: triapine|Drug: cisplatin|Radiation: external beam radiation therapy|Procedure: quality-of-life assessment|Other: questionnaire administration|Radiation: fludeoxyglucose F 18|Procedure: positron emission tomography|Procedure: computed tomography National Cancer Institute (NCI) Phase 2 2009-07-01 2014-04-21
    NCT00078975 Pancreatic Cancer Drug: gemcitabine hydrochloride|Drug: triapine University Health Network, Toronto|National Cancer Institute (NCI) Phase 2 2004-04-01 2016-06-21
    NCT02466971 Cervical Adenocarcinoma|Cervical Adenosquamous Carcinoma|Cervical Squamous Cell Carcinoma, Not Otherwise Specified|Stage IB2 Cervical Cancer|Stage II Vaginal Cancer|Stage IIA Cervical Cancer|Stage IIB Cervical Cancer|Stage III Vaginal Cancer|Stage IIIB Cervical Cancer|Stage IVA Cervical Cancer|Stage IVA Vaginal Cancer|Stage IVB Vaginal Cancer Drug: Cisplatin|Radiation: External Beam Radiation Therapy|Radiation: Intensity-Modulated Radiation Therapy|Radiation: Internal Radiation Therapy|Other: Laboratory Biomarker Analysis|Radiation: Radiation Therapy|Drug: Triapine National Cancer Institute (NCI) Phase 2 2016-01-01 2017-03-23
    NCT00381550 Accelerated Phase Chronic Myelogenous Leukemia|Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative|Blastic Phase Chronic Myelogenous Leukemia|Chronic Eosinophilic Leukemia|Chronic Myelomonocytic Leukemia|Essential Thrombocythemia|Philadelphia Chromosome Negative Chronic Myelogenous Leukemia|Polycythemia Vera|Primary Myelofibrosis|Relapsing Chronic Myelogenous Leukemia Drug: fludarabine phosphate|Drug: triapine|Procedure: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2006-08-01 2014-12-16
    NCT00075660 Kidney Cancer Drug: triapine NCIC Clinical Trials Group|National Cancer Institute (NCI)|Canadian Cancer Trials Group Phase 2 2004-01-01 2010-11-07
    NCT00006218 Unspecified Adult Solid Tumor, Protocol Specific Drug: triapine Vion Pharmaceuticals|National Cancer Institute (NCI) Phase 1 2000-05-01 2013-07-17

    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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