For research use only.

Catalog No.S7470 Synonyms: 3-AP

7 publications

Triapine Chemical Structure

CAS No. 200933-27-3

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

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Selleck's Triapine has been cited by 7 publications

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  • (a) Quantification of p-RPA/ Rad51, 53BP1 and γH2AX in GBM01 cells treated with DMSO or triapine. (b) Quantification of p-RPA/Rad51, 53BP1 and γH2AX in GBM02 cells treated with DMSO or triapine.

    Nat Commun, 2016, 7:13398. Triapine purchased from Selleck.

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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.
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SK-N-MC cells  NIPjXZRRem:uaX\ldoF1cW:wIHHzd4F6 NX\TNnBVPzJiaB?= MoGwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3OMW1EKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6yOkDPxE1? MVSxO|YxOjZyMx?=
human HCT116 cells NEXTeJlEgXSxdH;4bYNqfHliYYPzZZk> MnnMPVYhcA>? NYWwUpdETGG{azDjfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGVicEWzJIFnfGW{IEm2JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT6yNlYh|ryP MXGyOFkxODh|Nx?=
KB-3-1 cells MlW5R5l1d3SxeHnjbZR6KGG|c3H5 MXK3NkBp MlzFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVE1oeC2wZXfheIl3\SCNQj2zMVEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zLkSg{txO MYixPVM6PzN{Mh?=
KBV1 cells NFPDTHhEgXSxdH;4bYNqfHliYYPzZZk> MV[3NkBp MkfBR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVE1odHmlb4Dyc5RmcW5vZYjwdoV{e2mwZzDLRnYyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NT65JO69VQ>? NYfzb3dWOTl|OUezNlI>
HCT116 cells NVfIRppGTnWwY4Tpc44h[XO|YYm= NWTydWVXPCEQvF2= NXfuWJp4OjRiaB?= NUfpe2k1UW6mdXP0bY9vKG:oIGLPV{Bo\W6ncnH0bY9vKGmwIHj1cYFvKEiFVEGxOkBk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBxPTNiYYSgOEB2VSCjZoTldkAzPCCqcoOgZpkhe3CnY4Tyc5Bpd3SxbXX0dpk> NEDNPW0zPDlyMEizOy=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-Chk1 / Chk1 / p-CDK1/2 / CDK1/2 / p-H1 ; 

PubMed: 24413181     

NTC and BRCA1-kd SKOV-3 cells were treated with 5 μM olaparib, 0.75 μM triapine, or both agents in combination for 24 hr. Total protein was analyzed for the levels of phosphorylated and total Chk1, Cdk1/2, and histone H1 proteins by western blotting. 

Growth inhibition assay
Cell viability; 

PubMed: 31118677     

786-O and 769-P cells were treated with 0.5, 1, or 2 μM Triapine for 24, 48, and 72 hours respectively. The cell viability was assessed by CCK-8 assay. 

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]


Kinase Assay:


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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 Research:


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  • 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.

    (Only for Reference)
Animal Research:


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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL (102.43 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.

* 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.

Chemical Information

Molecular Weight 195.24


CAS No. 200933-27-3
Storage powder
in solvent
Synonyms 3-AP
Smiles C1=CC(=C(N=C1)C=NNC(=S)N)N

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% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04234568 Recruiting Drug: Lutetium Lu 177 Dotatate|Drug: Triapine Digestive System Neuroendocrine Tumor|Metastatic Well Differentiated Neuroendocrine Neoplasm National Cancer Institute (NCI) June 29 2020 Phase 1
NCT00293345 Completed Drug: gemcitabine hydrochloride|Drug: triapine 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID