Triapine

Catalog No.S7470 Synonyms: 3-AP

Triapine Chemical Structure

Molecular Weight(MW): 195.24

Triapine is a potent ribonucleotide reductase inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2.

Size Price Stock Quantity  
USD 97 In stock
USD 237 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 2 Publications

1 Customer Review

  • (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.

Purity & Quality Control

Choose Selective DNA/RNA Synthesis Inhibitors

Biological Activity

Description Triapine is a potent ribonucleotide reductase 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SK-N-MC cells  M1XxenBzd2yrZnXyZZRqd25iYYPzZZk> MX23NkBp MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV6tUWMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkK2JO69VQ>? NWewRolsOTd4MEK2NFM>
human HCT116 cells NVvOb3h7S3m2b4TvfIlkcXS7IHHzd4F6 M1niUlk3KGh? Mln3SIFzcyCleYTveI95cWOrdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOg[ZhxemW|c3nu[{B4cWymIIT5dIUheDV|IHHmeIVzKDl4IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OS5{Mk[g{txO NG\4c3UzPDlyMEizOy=>
KB-3-1 cells NV;lOmF1S3m2b4TvfIlkcXS7IHHzd4F6 M{nkd|czKGh? MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQMYdxNW6nZ3H0bZZmKEuELUOtNUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFwNDFOwG0> M1jEWFE6Ozl5M{Ky
KBV1 cells MV\DfZRwfG:6aXPpeJkh[XO|YYm= M1HIN|czKGh? M13TZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHAu\2y7Y3;wdo91\WmwLXX4dJJme3OrbnegT2JXOSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUWuPUDPxE1? MkfxNVk{QTd|MkK=
HCT116 cells Mo\VSpVv[3Srb36gZZN{[Xl? NIna[Io1KM7:TR?= NEPYdVUzPCCq M1vJWmlv\HWldHnvckBw\iCUT2Og[4Vv\XKjdHnvckBqdiCqdX3hckBJS1RzMU[gZ4VtdHNiZYjwdoV{e2mwZzD3bYxlKHS7cHWgdFU{KGG2IESgeW0h[W[2ZYKgNlQhcHK|IHL5JJNx\WO2cn;wbI91d22ndIL5 NUeyXZV6OjR7MEC4N|c>

... Click to View More Cell Line Experimental Data

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

Kinase Assay:

[1]

+ Expand

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:

[1]

+ Expand
  • 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:

[1]

+ Expand
  • 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.
  • Formulation: 0.9% NaCl or water
  • 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):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.
1.25mg/mL

* 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
Formula

C7H9N5S

CAS No. 200933-27-3
Storage powder
in solvent
Synonyms 3-AP

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

DNA/RNA Synthesis Signaling Pathway Map

Related DNA/RNA Synthesis Products

Tags: buy Triapine | Triapine supplier | purchase Triapine | Triapine cost | Triapine manufacturer | order Triapine | Triapine distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID