Triapine (3-AP)

Catalog No.S7470 Batch:S747002

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Technical Data

Formula

C7H9N5S
Molecular Weight 195.24 CAS No. 200933-27-3
Solubility (25°C)* In vitro 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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 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]

Protocol (from reference)

Kinase Assay:

[1]
  • 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.
Cell Assay:

[1]
  • Cell lines

    Wild-type KB and HU-resistant KB nasopharyngeal carcinoma cells.

  • Concentrations

    ~10 μM

  • Incubation Time

    A period of 3 generations

  • Method

    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.
Animal Study:

[1]
  • Animal Models

    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.

  • Dosages

    ~24 mg/kg

  • Administration

    i.p. or i.v.

Customer Product Validation

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

Selleck's Triapine (3-AP) has been cited by 16 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.