Triapine (3-AP)

製品コードS7470 バッチS747002

印刷

化学情報

Chemical Structure Synonyms Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C7H9N5S
分子量 195.24 CAS No. 200933-27-3
Solubility (25°C)* 体外 DMSO 39 mg/mL (199.75 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
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]
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 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.
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.
投薬量 ~24 mg/kg
投与方法 i.p. or i.v.

カスタマーフィードバック

Data from [Data independently produced by , , Nat Commun, 2016, 7:13398]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Critical role for ribonucleoside-diphosphate reductase subunit M2 in ALV-J-induced activation of Wnt/β-catenin signaling via interaction with P27 [ J Virol, 2023, 97(8):e0026723] PubMed: 37582207
Elevated glucose promotes DNA replication and cancer cell growth through pRB-E2F1 [ Res Sq, 2023, rs.3.rs-3126261] PubMed: 37502888
Targeting Ribonucleotide Reductase Induces Synthetic Lethality in PP2A-Deficient Uterine Serous Carcinoma [ Cancer Res, 2022, 82(4):721-733] PubMed: 34921012
Yap is essential for uterine decidualization through Rrm2/GSH/ROS pathway in response to Bmp2 [ Int J Biol Sci, 2022, 18(6):2261-2276] PubMed: 35414789
A modular master regulator landscape controls cancer transcriptional identity [ Cell, 2021, 184(2):334-351.e20] PubMed: 33434495
Translational evidence for RRM2 as a prognostic biomarker and therapeutic target in Ewing sarcoma [ Mol Cancer, 2021, 20(1):97] PubMed: 34315482
Control of replication stress and mitosis in colorectal cancer stem cells through the interplay of PARP1, MRE11 and RAD51 [ Cell Death Differ, 2021, 10.1038/s41418-020-00733-4] PubMed: 33531658
De novo deoxyribonucleotide biosynthesis regulates cell growth and tumor progression in small-cell lung carcinoma [ Sci Rep, 2021, 11(1):13474] PubMed: 34188151
Association Between Iron and Cholesterol in Neuroblastomas [ Anticancer Res, 2021, 41(6):2795-2804] PubMed: 34083269
The lncRNAlincNMRregulates nucleotide metabolism via a YBX1 - RRM2 axis in cancer [ Nature Communications, 2020, 3214-2020)] PubMed: None

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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