Triapine (3-AP)
Triapine (3-AP) 是一种强效的ribonucleotide reductase (RNR)抑制剂，通过抑制DNA的合成而具有广谱抗肿瘤活性。
Triapine (3-AP) Chemical Structure
CAS: 200933-27-3
产品质控
批次：
纯度：
99.92%
99.92
Triapine (3-AP)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HCT116 | Function assay | 4 uM | 24 hrs | Induction of ROS generation in human HCT116 cells expressing wild type p53 at 4 uM after 24 hrs by spectrophotometry | 24900837 |
| SW480 | Function assay | 2.5 uM | 48 hrs | Induction of morphological changes in human SW480 cells assessed as induction of massive cell flattening at 2.5 uM incubated for 48 hrs by phase contrast microscopy | 27336684 |
| HL60 | Function assay | 1 and 5 uM | 30 mins | Induction of intracellular ROS generation in human HL60 cells at 1 and 5 uM in presence of CuCl2 incubated for 30 mins by DCF-DA staining based fluorescence assay | 27336684 |
| SK-N-MC | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay, IC50=0.26μM | 17602603 | |
| KB-3-1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay, IC50=1.4μM | 19397322 | |
| KB-3-1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay, IC50=1.41254μM | 19397322 | |
| KBV1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay, IC50=5.88844μM | 19397322 | |
| KBV1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay, IC50=5.9μM | 19397322 | |
| SK-N-MC | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay, IC50=0.26μM | 19601577 | |
| HCT116 | Dark cytotoxicity assay | 96 hrs | Dark cytotoxicity against human HCT116 cells expressing wild type p53 after 96 hrs by MTT assay, IC50=1.226μM | 24900837 | |
| HCT116 | Photocytotoxicity assay | 24 hrs | Photocytotoxicity against human HCT116 cells expressing wild type p53 incubated for 24 hrs followed by light irradiation measured after 24 hrs by MTS assay in presence of ALA and FeCl3 | 24900837 | |
| KB-3-1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay, IC50=3.1μM | 27336684 | |
| KBC1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human KBC1 cells incubated for 72 hrs by MTT assay, IC50=8.9μM | 27336684 | |
| WPMY-1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human WPMY-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay, IC50=4.96μM | 31614257 | |
| GES-1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human GES-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay, IC50=5.6μM | 31614257 | |
| GES-1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human GES-1 cells after 72 hrs by MTT assay, IC50=5.4μM | ChEMBL | |
| MGC803 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay, IC50=9.68μM | ChEMBL | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=18.85μM | ChEMBL | |
| SMMC7721 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay, IC50=42.81μM | ChEMBL | |
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 18159922 | ||
| SK-N-MC | Antiproliferative assay | Antiproliferative activity against human SK-N-MC cells by MTT assay, IC50=0.54μM | 17963372 | ||
| SK-N-MC | Antiproliferative assay | Antiproliferative activity against human SK-N-MC cells by MTT assay, IC50=0.31μM | 17142046 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 27336684 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 27336684 | ||
| L1210 | Growth inhibition assay | Growth inhibition of mouse L1210 cells by MTS assay, IC50=1.3μM | 30904782 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 31614257 | ||
| HEK293 | Cytotoxicity assay | Cytotoxicity against HEK293 cells (CO-ADD:MA_007); CC50 by cell viability assay in DMEM (10% FBS) media using TC plates, by Resazurin F(560/590), CC50=2.827μM | ChEMBL | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Triapine (3-AP) 是一种强效的ribonucleotide reductase (RNR)抑制剂，通过抑制DNA的合成而具有广谱抗肿瘤活性。 | |
|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在野生型KB和HU-抗性KB的鼻咽癌细胞中，Triapine抑制核苷酸还原酶的活性。在一系列的肿瘤细胞系中，Triapine通过抑制DNA合成具有广谱的抗肿瘤活性。[1]在体外实验中，Triapine阻断缺血性的神经毒性和低氧毒性，其EC50分别是0.35 μM 和 0.75 μM。Triapine通过抑制神经毒剂，包括星状孢菌素，藜芦定和 谷氨酸等诱导的细胞死亡，表现出神经保护活性。[2] | |||
|---|---|---|---|---|
| 激酶实验 | 核糖核苷酸还原酶实验 | |||
| CDP还原酶通过Dowex 1-borate离子交换色谱测定。实验体系包含0.02 μCi [14C]CDP (52.9 mCi/mmol), 3 mM 二硫苏糖醇，6 mM MgCl2，30 mM HEPES，5 mM ATP，0.15 mM 未标记的CDP，以及10 μL 细胞提取物，终体积为0.02 毫升。反应的培养时间为60分钟，反应和时间呈线性关系。 | ||||
| 细胞实验 | 细胞系 | 野生型KB和HU抵性KB鼻咽癌 | ||
| 浓度 | ~10 μM | |||
| 孵育时间 | 第3代时期 | |||
| 方法 | 细胞以104每孔的密度接种于24孔板上，药物加入到细胞中，连续培养3代（未经处理的对照细胞），随后用亚甲基蓝试验测定细胞生长。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-Chk1 / Chk1 / p-CDK1/2 / CDK1/2 / p-H1 |
|
24413181 | |
| Growth inhibition assay | Cell viability |
|
31118677 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在有L1210白血病的小鼠中，Triapine (1.25~20 毫克/千克)能够治疗一些小鼠且没有致命毒性。Triapine同时抑制小鼠M109 肺癌和人 A2780 卵巢癌的肿瘤生长。此外，联合使用Triapine和其它的损伤DNA的抑制剂能够对L1210 白血病协同抑制。[1]在大鼠瞬时缺血模型中，当(50 μ 每只大鼠)注射时，Triapine 减少59%的梗死体积，静脉注射(1 毫克/千克)时，减少35%的梗死体积。[2] | |
|---|---|---|
| 动物实验 | Animal Models | 患有L1210白血病和 M109肺肿瘤的BALB/cBA/2 (CD2F1)小鼠，异种移植人A2780卵巢癌的无胸腺nu/nu小鼠。 |
| Dosages | ~24毫克/千克 | |
| Administration | 腹腔注射或静脉注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00293345 | Completed | 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|Waldenström Macroglobulinemia |
National Cancer Institute (NCI) |
June 2006 | Phase 1 |
化学信息&溶解度
| 分子量 | 195.24 | 分子式 | C7H9N5S |
| CAS号 | 200933-27-3 | SDF | Download Triapine (3-AP) SDF |
| Smiles | C1=CC(=C(N=C1)C=NNC(=S)N)N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 39 mg/mL ( (199.75 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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