Triapine (3-AP)

製品コード：S7470 純度：99.92%

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

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
10mg	JPY 22000	国内在庫あり
100mg	JPY 101800	国内在庫なし(納期7~10日)
1g	JPY 298500	国内在庫なし(納期7~10日)

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Triapine (3-AP)関連製品

関連ターゲット	tRNA synthetase RdRp DNA synthesis helicase ribonucleotide reductase	もっと見る
関連製品	Pidnarulex (CX-5461) SCR7 Favipiravir (T-705) RK-33 Carmofur B02 BMH-21 YK-4-279 Bergapten Tegafur (FT-207) Azaguanine-8 Halofuginone Adenine HCl Mizoribine Cyclocytidine HCl Thymidine APX-3330 Nedaplatin 6-Thio-dG Flupirtine maleate JH-RE-06 Pritelivir (BAY 57-1293) TK216 Amenamevir Madrasin Tubercidin BC-LI-0186 CRT0044876 PFM01 Adenine ML216	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

DNA/RNA Synthesisシグナル伝達経路

DNA/RNA Synthesis阻害剤の選択性比較

阻害剤	Citation	tRNA synthetase	RdRp	DNA synthesis	helicase	YB-1	ribonucleotide reductase	ribonucleotide reductase	PCNA	その他
ART899	0
ART812	0
ART558	0
SU056	2					+
VV116	0		+
BC-LI-0186	1	+++
Acelarin (NUC-1031)	0			++++
Suramin sodium salt	1		++							SirT1,SirT2,Topoisomerase II
ML216	3				+
Halofuginone	11	+++								Smad3
Clevudine	1
Nedaplatin	3			✔
Triapine (3-AP)	17						✔	✔
RP-6685	0
H3B-8800	0
Basic Orange 14	0
AOH1996	0								✔
Didox	0						✔	✔
Phen-DC3 Trifluoromethanesulfonate	0				✔
Robinetin	0			✔
Metarrestin	0									PNC
Brr2 Inhibitor C9	0				✔
Triglycidyl Isocyanurate (Teroxirone)	0			✔						p53
RK-33	21				✔
Oxolinic acid	0			✔						bacterial DNA gyrase,dopamine uptake
Favipiravir (T-705)	24		✔
YK-4-279	14				✔
Blasticidin S HCl	29			✔						protein synthesis
CX-3543(Quarfloxin)	0

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

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
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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
Kinase 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
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考
[1] Finch RA, et al. Biochem Pharmacol. 2000, 59(8), 983-991. [2] Jiang ZG, et al. CNS Drug Rev. 2006, 12(1), 77-90.

参考

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	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

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

Clear solution

5%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O

1.25mg/ml (6.40mM)

Taking the 1 mL working solution as an example, add 50 μL 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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