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Triapine (3-AP)
Triapine (3-AP) 是一種強效的ribonucleotide reductase (RNR)抑制劑，通過抑制DNA的合成而具有廣譜抗腫瘤活性。
Triapine (3-AP) Chemical Structure
CAS: 200933-27-3
產(chǎn)品質控
批次：
純度：
99.92%
99.92
Triapine (3-AP)相關產(chǎn)品
相關信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Triapine (3-AP) 是一種強效的ribonucleotide reductase (RNR)抑制劑，通過抑制DNA的合成而具有廣譜抗腫瘤活性。 | |
|---|---|---|
| 靶點 |
|
| 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|Waldenstr?m Macroglobulinemia |
National Cancer Institute (NCI) |
June 2006 | Phase 1 |
化學信息&溶解度
| 分子量 | 195.24 | 分子式 | C7H9N5S |
| CAS號 | 200933-27-3 | SDF | Download Triapine (3-AP) SDF |
| Smiles | C1=CC(=C(N=C1)C=NNC(=S)N)N | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 39 mg/mL ( (199.75 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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