Triapine
Based on 11 publication(s) in Google Scholar
Triapine (3-AP; PAN-811) is a potent inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer.
For research use only. We do not sell to patients.
- Purity: 99.78%
- CAS No.: 143621-35-6
- Formula: C7H9N5S
- Molecular Weight:195.24
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Triapine
More- Nature. 2025 Jul;643(8070):192-200. [Abstract]
- Cell Death Dis. 2026 Feb 26;17(1):275. [Abstract]
- Cancer Lett. 2024 Aug 1:596:216993. [Abstract]
- JACS Au. 2024 Dec 4;4(12):4799-4808. [Abstract]
- mBio. 2025 Aug 13;16(8):e0104725. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- J Cancer Res Clin Oncol. 2023 Sep;149(11):8605-8617. [Abstract]
- Res Sq. 2026 Jun 17.
- Rush University. 2025.
- Res Sq. 2025 Mar 26.
- Research Square Preprint. 2023 Jun 9.
All DNA/RNA Synthesis Isoforms
More
Biological Activity
Ribonucleotide reductase (RR)[1]
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.7 μM
Compound: Triapine
|
Cytotoxicity against human A2780 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human A2780 cells incubated for 72 hrs by MTT assay
|
[PMID: 27336684] |
| A549 | IC50 |
2.288 μM
Compound: 3-AP
|
Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| BGC-823 | IC50 |
3.07 μM
Compound: 3-AP
|
Antiproliferative activity against human BGC-823 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human BGC-823 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| EC9706 | IC50 |
3.084 μM
Compound: 3-AP
|
Antiproliferative activity against human EC9706 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human EC9706 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| GES1 | IC50 |
5.4 μM
Compound: 3-AP
|
Cytotoxicity against human GES-1 cells after 72 hrs by MTT assay
Cytotoxicity against human GES-1 cells after 72 hrs by MTT assay
|
[PMID: 30108734] |
| GES1 | IC50 |
5.6 μM
Compound: 3-AP
|
Antiproliferative activity against human GES-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human GES-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay
|
[PMID: 31614257] |
| GES1 | IC50 |
6.103 μM
Compound: 3-AP
|
Cytotoxicity against human GES1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human GES1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| HCT-116 | IC50 |
1.226 μM
Compound: II
|
Dark cytotoxicity against human HCT116 cells expressing wild type p53 after 96 hrs by MTT assay
Dark cytotoxicity against human HCT116 cells expressing wild type p53 after 96 hrs by MTT assay
|
[PMID: 24900837] |
| HGC-27 | IC50 |
11.495 μM
Compound: 3-AP
|
Antiproliferative activity against human HGC-27 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HGC-27 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| HUVEC | IC50 |
3448 nM
Compound: 3-AP
|
Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay
Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay
|
[PMID: 30835473] |
| KB 3-1 | IC50 |
>800 μM
Compound: 3-AP
|
Antiproliferative activity against human KB3-1 cells after 24 hrs by MTT assay
Antiproliferative activity against human KB3-1 cells after 24 hrs by MTT assay
|
[PMID: 27524608] |
| KB 3-1 | IC50 |
>800 μM
Compound: 3-AP
|
Antiproliferative activity against human KB3-1 cells after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay
Antiproliferative activity against human KB3-1 cells after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay
|
[PMID: 27524608] |
| KB 3-1 | IC50 |
1.4 μM
Compound: 9
|
Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay
Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay
|
[PMID: 19397322] |
| KB 3-1 | IC50 |
3.1 μM
Compound: Triapine
|
Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay
|
[PMID: 27336684] |
| KB-V1 | IC50 |
>800 μM
Compound: 3-AP
|
Antiproliferative activity against human KBV1 cells over expressing P-gp after 24 hrs by MTT assay
Antiproliferative activity against human KBV1 cells over expressing P-gp after 24 hrs by MTT assay
|
[PMID: 27524608] |
| KB-V1 | IC50 |
>800 μM
Compound: 3-AP
|
Antiproliferative activity against human KBV1 cells over expressing P-gp after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay
Antiproliferative activity against human KBV1 cells over expressing P-gp after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay
|
[PMID: 27524608] |
| KB-V1 | IC50 |
5.9 μM
Compound: 9
|
Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay
Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay
|
[PMID: 19397322] |
| L1210 | IC50 |
1.3 μM
Compound: 1; 3-AP
|
Growth inhibition of mouse L1210 cells by MTS assay
Growth inhibition of mouse L1210 cells by MTS assay
|
[PMID: 30904782] |
| MCF7 | IC50 |
>32 μM
Compound: 3-AP
|
Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| MCF7 | IC50 |
18.85 μM
Compound: 3-AP
|
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
|
[PMID: 30108734] |
| MES-SA | IC50 |
1.305 μM
Compound: Triapine
|
Cytotoxicity against human MES-SA cells transfected with mCherry fluorescent protein assessed as inhibition of cell proliferation incubated for 72 hrs by fluorescent assay
Cytotoxicity against human MES-SA cells transfected with mCherry fluorescent protein assessed as inhibition of cell proliferation incubated for 72 hrs by fluorescent assay
|
[PMID: 27161177] |
| MES-SA/Dx5 | IC50 |
2.523 μM
Compound: Triapine
|
Cytotoxicity against human MES-SA/DX5 cells transfected with mCherry fluorescent protein assessed as inhibition of cell proliferation incubated for 72 hrs by fluorescent assay
Cytotoxicity against human MES-SA/DX5 cells transfected with mCherry fluorescent protein assessed as inhibition of cell proliferation incubated for 72 hrs by fluorescent assay
|
[PMID: 27161177] |
| MGC-803 | IC50 |
5.411 μM
Compound: 3-AP
|
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| MGC-803 | IC50 |
9.68 μM
Compound: 3-AP
|
Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay
Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay
|
[PMID: 30108734] |
| MV4-11 | IC50 |
967.6 nM
Compound: 3-AP
|
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay
|
[PMID: 30835473] |
| PC-3 | IC50 |
0.56 μM
Compound: 3-AP
|
Antiproliferative activity against human PC3 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay
|
[PMID: 31614257] |
| PC-3 | IC50 |
0.56 μM
Compound: 3-AP
|
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 33153765] |
| SGC-7901 | IC50 |
18.349 μM
Compound: 3-AP
|
Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
|
[PMID: 32438199] |
| SK-N-MC | IC50 |
0.26 μM
Compound: 3-AP
|
Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
|
[PMID: 17602603] |
| SK-N-MC | IC50 |
0.26 μM
Compound: 3-AP
|
Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
|
[PMID: 19601577] |
| SK-N-MC | IC50 |
0.31 μM
Compound: triapine
|
Antiproliferative activity against human SK-N-MC cells by MTT assay
Antiproliferative activity against human SK-N-MC cells by MTT assay
|
[PMID: 17142046] |
| SK-N-MC | IC50 |
0.54 μM
Compound: 3-AP
|
Antiproliferative activity against human SK-N-MC cells by MTT assay
Antiproliferative activity against human SK-N-MC cells by MTT assay
|
[PMID: 17963372] |
| SMMC-7721 | IC50 |
42.81 μM
Compound: 3-AP
|
Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay
Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay
|
[PMID: 30108734] |
| SW480 | IC50 |
>50 μM
Compound: Triapine
|
Cytotoxicity against triapine-resistant human SW480 cells incubated for 72 hrs by MTT assay
Cytotoxicity against triapine-resistant human SW480 cells incubated for 72 hrs by MTT assay
|
[PMID: 27336684] |
| SW480 | IC50 |
0.84 μM
Compound: Triapine
|
Cytotoxicity against human SW480 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human SW480 cells incubated for 72 hrs by MTT assay
|
[PMID: 27336684] |
| WI-38 | IC50 |
>25 μM
Compound: Triapine
|
Cytotoxicity against human WI38 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human WI38 cells incubated for 72 hrs by MTT assay
|
[PMID: 27336684] |
Triapine (3-AP; PAN-811) is a potent derivative of α-heterocyclic carboxaldehyde thiosemicarbazone (HCT) that inhibits hRRM2 and p53R2 isoforms of the M2 subunit[1]. Triapine (3-AP; PAN-811) is thought to inhibit ribonucleotide reductase through its preformed iron chelate, rather than directly by removing iron from the active site. In cells containing less topoisomerase IIα fewer DNA strand breaks will be produced, and thus topoisomerase II poisons will be less inhibitory in the K/VP.5 cell line. The IC50s for Dp44mT growth inhibition are 48±9 nM and 60±12 nM, for K562 and K/VP.5 cells, respectively. The IC50s for Triapine growth inhibition are 476±39 nM and 661±69 nM for K562 and K/VP.5 cells, respectively[2]. PKIH and DpT Fe chelators show high antiproliferative activity against a range of tumor cell lines. Dp44mT shows the greatest antitumor efficacy with an IC50 that ranged from 0.005 to 0.4 μM. The average IC50 of Dp44mT over 28 cell types is 0.03±0.01 μM, which is significantly lower than that of Triapine (3-AP; PAN-811; average IC50: 1.41±0.37 μM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 143621-35-6
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Appearance Solid
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Molecular Weight 195.24
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Formula C7H9N5S
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Color Light yellow to khaki
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SMILES
S=C(N)N/N=C/C1=NC=CC=C1N
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Synonyms
3-AP; PAN-811; OCX191
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (11)
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Journal Impact Factor
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Most Recent
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Nature
2025 Jul;643(8070):192-200. PMID: 39695227 -
Cell Death Dis
2026 Feb 26;17(1):275. PMID: 41748545 -
Cancer Lett
Inhibition of Ribonucleotide Reductase Subunit M2 Enhances the Radiosensitivity of Metastatic Pancreatic Neuroendocrine Tumor. [Abstract]2024 Aug 1:596:216993. PMID: 38801884 -
JACS Au
2024 Dec 4;4(12):4799-4808. PMID: 39735911 -
mBio
Blockade of de novo dNTP biosynthesis pathway delays HIV-1 early life cycle kinetics and dynamics. [Abstract]2025 Aug 13;16(8):e0104725. PMID: 40586616 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
J Cancer Res Clin Oncol
Synergistic anticancer activity of combined ATR and ribonucleotide reductase inhibition in Ewing's sarcoma cells. [Abstract]2023 Sep;149(11):8605-8617. PMID: 37097390 -
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Solvent & Solubility
DMSO : ≥ 47 mg/mL (240.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (12.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (12.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
An MTT assay is used to determine cell growth inhibition of CHO cells. Human leukemia K562 cells and K/VP.5 cells (a 26-fold etoposide-resistant K562-derived sub-line with decreased levels of topoisomerase IIα mRNA and protein) are maintained as suspension cultures in MEM containing 10% fetal calf serum (FCS). For growth inhibition assays, K562 and K/VP.5 cells are plated at a concentration of 1.5×105 cell/mL, and incubated 5 d with various concentrations of Dp44mT, Triapine or vehicle (DMSO) for 48 h, after which cells are counted on a model ZBF Coulter counter. The IC50 growth inhibitory concentration for each cell line is calculated from a non-linear least-squares fit to a 2-parameter logistic equation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
Female BALB/c nu/nu mice are used at 8-10 weeks of age. Tumor cells in culture are harvested, and 107 cells are suspended in Matrigel and injected s.c. into the right flanks of mice. After engraftment, tumor size is measured by Vernier calipers. Tumor volumes (in cubic millimeters) are calculated. When tumor volumes reached 120 mm3, i.v. treatment began (day 0). Chelators (e.g., Triapine) are dissolved in 15% propylene glycol in 0.9% saline and injected i.v. over 5 consecutive days per week for up to 7 weeks. Control mice are treated with vehicle alone.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
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Handling Instructions (2659 KB)
References
[1]. Martin LK, et al. A dose escalation and pharmacodynamic study of Triapine and radiation in patients with locally advanced pancreas cancer. Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e475-81. [Content Brief]
[2]. Yalowich JC, et al. The anticancer thiosemicarbazones Dp44mT and Triapine lack inhibitory effects as catalytic inhibitors or poisons of DNA topoisomerase IIα. Biochem Pharmacol. 2012 Jul 1;84(1):52-8. [Content Brief]
[3]. Whitnall M, et al. A class of iron chelators with a wide spectrum of potent antitumor activity that overcomes resistance to chemotherapeutics. Proc Natl Acad Sci U S A. 2006 Oct 3;103(40):14901-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.1219 mL | 25.6095 mL | 51.2190 mL | 128.0475 mL |
| 5 mM | 1.0244 mL | 5.1219 mL | 10.2438 mL | 25.6095 mL | |
| 10 mM | 0.5122 mL | 2.5610 mL | 5.1219 mL | 12.8048 mL | |
| 15 mM | 0.3415 mL | 1.7073 mL | 3.4146 mL | 8.5365 mL | |
| 20 mM | 0.2561 mL | 1.2805 mL | 2.5610 mL | 6.4024 mL | |
| 25 mM | 0.2049 mL | 1.0244 mL | 2.0488 mL | 5.1219 mL | |
| 30 mM | 0.1707 mL | 0.8537 mL | 1.7073 mL | 4.2683 mL | |
| 40 mM | 0.1280 mL | 0.6402 mL | 1.2805 mL | 3.2012 mL | |
| 50 mM | 0.1024 mL | 0.5122 mL | 1.0244 mL | 2.5610 mL | |
| 60 mM | 0.0854 mL | 0.4268 mL | 0.8537 mL | 2.1341 mL | |
| 80 mM | 0.0640 mL | 0.3201 mL | 0.6402 mL | 1.6006 mL | |
| 100 mM | 0.0512 mL | 0.2561 mL | 0.5122 mL | 1.2805 mL |