Triapine (3-AP)

Triapine (3-AP) is a potent ribonucleotide reductase (RNR) inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2.

Triapine (3-AP)化学構造

CAS No. 200933-27-3

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 101800 国内在庫なし(納期7~10日)
JPY 298500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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製品安全説明書

現在のバッチを見る: 純度: 99.92%
99.92

Triapine (3-AP)関連製品

DNA/RNA Synthesis阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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生物活性

製品説明 Triapine (3-AP) is a potent ribonucleotide reductase (RNR) inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2.
Targets
Ribonucleotide reductase [1]
In Vitro
In vitro Triapine potently inhibits the activity of ribonucleotide reductase in both wild-type KB and HU-resistant KB nasopharyngeal carcinoma cells. Triapine shows broad spectrum antitumor activity by inhibiting DNA synthesis in a series of cancer cell lines. [1] In vitro, Triapine blocks ischemic neurotoxicity and hypoxic toxicity with EC50 of 0.35 μM and 0.75 μM, respectively. Triapine also shows its neuroprotective activity by suppressing cell death induced by neurotoxic agents, including staurosporine, veratridine and glutamate. [2]
Kinase Assay Ribonucleotide reductase assay
CDP reductase is assayed using Dowex 1-borate ion-exchange chromatography. The assay mixture contains 0.02 μCi of [14C]CDP (52.9 mCi/mmol), 3 mM dithiothreitol, 6 mM MgCl2, 30 mM HEPES, 5 mM ATP, 0.15 mM unlabeled CDP, and 10 μL of cellular extract in a final volume of 0.02 mL. The incubation time for the reaction is 60 min, during which time the reaction is linear.
細胞実験 細胞株 Wild-type KB and HU-resistant KB nasopharyngeal carcinoma cells.
濃度 ~10 μM
反応時間 A period of 3 generations
実験の流れ

Cells are plated at a density of 104 cells/mL per well in 24-well plates. Drugs are added to cells and incubations are continued for a period of 3 generations (untreated control cells), followed by assessment of cell growth by the methylene blue assay.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-Chk1 / Chk1 / p-CDK1/2 / CDK1/2 / p-H1 24413181
Growth inhibition assay Cell viability 31118677
In Vivo
In Vivo In mice bearing the L1210 leukemia, Triapine (1.25 to 20 mg/kg) is curative for some mice without lethal toxicity. Triapine also inhibits the growth of solid tumors in mice M109 lung carcinoma and human A2780 ovarian carcinoma xenografts. In addition, combination of Triapine with various classes of agents that damage DNA results in synergistic inhibition of the L1210 leukemia. [1] In a rat model of transient ischemia, Triapine reduces infarct volume by 59% when administered i.c.v. (50 μ per rat) and by 35% when administered i.v. (1 mg/kg). [2]
動物実験 動物モデル BALB/cBA/2 (CD2F1) mice with the L1210 leukemia and the M109 lung carcinoma, athymic nu/nu mice with the human A2780 ovarian carcinoma xenograft.
投与量 ~24 mg/kg
投与経路 i.p. or i.v.
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

化学情報

分子量 195.24 化学式

C7H9N5S

CAS No. 200933-27-3 SDF Download Triapine (3-AP) SDFをダウンロードする
Smiles C1=CC(=C(N=C1)C=NNC(=S)N)N
保管

In vitro
Batch:

DMSO : 39 mg/mL ( (199.75 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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