Name: Triapine (3-AP)
Brand: Selleck Chemicals
SKU: S7470
Rating: 5 (18 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.92%

99.92

Gerelateerde doelwitten	HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF
Overige DNA/RNA Synthesis Inhibitoren	CX-5461 (Pidnarulex) SCR7 Favipiravir (T-705) RK-33 EED226 BMH-21 Carmofur YK-4-279 Halofuginone Tegafur (FT-207)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
SK-N-MC	Antiproliferative assay			Antiproliferative activity against human SK-N-MC cells by MTT assay, IC50=0.31μM	17142046
SK-N-MC	Antiproliferative assay		72 hrs	Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay, IC50=0.26μM	17602603
SK-N-MC	Antiproliferative assay			Antiproliferative activity against human SK-N-MC cells by MTT assay, IC50=0.54μM	17963372
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	18159922
KB-3-1	Cytotoxicity assay		72 hrs	Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay, IC50=1.4μM	19397322
KB-3-1	Cytotoxicity assay		72 hrs	Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay, IC50=1.41254μM	19397322
KBV1	Cytotoxicity assay		72 hrs	Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay, IC50=5.88844μM	19397322
KBV1	Cytotoxicity assay		72 hrs	Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay, IC50=5.9μM	19397322
SK-N-MC	Antiproliferative assay		72 hrs	Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay, IC50=0.26μM	19601577
HCT116	Dark cytotoxicity assay		96 hrs	Dark cytotoxicity against human HCT116 cells expressing wild type p53 after 96 hrs by MTT assay, IC50=1.226μM	24900837
HCT116	Photocytotoxicity assay		24 hrs	Photocytotoxicity against human HCT116 cells expressing wild type p53 incubated for 24 hrs followed by light irradiation measured after 24 hrs by MTS assay in presence of ALA and FeCl3	24900837
HCT116	Function assay	4 uM	24 hrs	Induction of ROS generation in human HCT116 cells expressing wild type p53 at 4 uM after 24 hrs by spectrophotometry	24900837
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	27336684
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	27336684
KB-3-1	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay, IC50=3.1μM	27336684
KBC1	Cytotoxicity assay		72 hrs	Cytotoxicity against human KBC1 cells incubated for 72 hrs by MTT assay, IC50=8.9μM	27336684
SW480	Function assay	2.5 uM	48 hrs	Induction of morphological changes in human SW480 cells assessed as induction of massive cell flattening at 2.5 uM incubated for 48 hrs by phase contrast microscopy	27336684
HL60	Function assay	1 and 5 uM	30 mins	Induction of intracellular ROS generation in human HL60 cells at 1 and 5 uM in presence of CuCl2 incubated for 30 mins by DCF-DA staining based fluorescence assay	27336684
L1210	Growth inhibition assay			Growth inhibition of mouse L1210 cells by MTS assay, IC50=1.3μM	30904782
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	31614257
WPMY-1	Antiproliferative assay		72 hrs	Antiproliferative activity against human WPMY-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay, IC50=4.96μM	31614257
GES-1	Antiproliferative assay		72 hrs	Antiproliferative activity against human GES-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay, IC50=5.6μM	31614257
HEK293	Cytotoxicity assay			Cytotoxicity against HEK293 cells (CO-ADD:MA_007); CC50 by cell viability assay in DMEM (10% FBS) media using TC plates, by Resazurin F(560/590), CC50=2.827μM	ChEMBL
GES-1	Cytotoxicity assay		72 hrs	Cytotoxicity against human GES-1 cells after 72 hrs by MTT assay, IC50=5.4μM	ChEMBL
MGC803	Antiproliferative assay		72 hrs	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay, IC50=9.68μM	ChEMBL
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=18.85μM	ChEMBL
SMMC7721	Antiproliferative assay		72 hrs	Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay, IC50=42.81μM	ChEMBL
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	195.24	Formule	C₇H₉N₅S	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	200933-27-3	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 39 mg/mL (199.75 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.250mg/ml (6.40mM)	Taking the 1 mL working solution as an example, add 50 μL 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	Ribonucleotide reductase
In vitro	Triapine (3-AP) potently inhibits the activity of ribonucleotide reductase in both wild-type KB and HU-resistant KB nasopharyngeal carcinoma cells, and shows broad spectrum antitumor activity by inhibiting DNA synthesis in a series of cancer cell lines. In vitro, it blocks ischemic neurotoxicity and hypoxic toxicity with EC50 of 0.35 μM and 0.75 μM, respectively. This compound also shows its neuroprotective activity by suppressing cell death induced by neurotoxic agents, including staurosporine, veratridine and glutamate.
Kinase Assay	Ribonucleotide reductase-test
Kinase Assay	CDP-reductase wordt getest met behulp van Dowex 1-boraat ionenuitwisselingschromatografie. Het testmengsel bevat 0,02 μCi [¹⁴C]CDP (52,9 mCi/mmol), 3 mM dithiothreitol, 6 mM MgCl₂, 30 mM HEPES, 5 mM ATP, 0,15 mM ongelabeld CDP en 10 μL cellulair extract in een eindvolume van 0,02 mL. De incubatietijd voor de reactie is 60 min, gedurende welke tijd de reactie lineair is.
In vivo	In mice bearing the L1210 leukemia, Triapine (3-AP) (1.25 to 20 mg/kg) is curative for some mice without lethal toxicity. This compound also inhibits the growth of solid tumors in mice M109 lung carcinoma and human A2780 ovarian carcinoma xenografts. In addition, its combination with various classes of agents that damage DNA results in synergistic inhibition of the L1210 leukemia. In a rat model of transient ischemia, it reduces infarct volume by 59% when administered i.c.v. (50 μ per rat) and by 35% when administered i.v. (1 mg/kg).
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/10692563/ [2] https://pubmed.ncbi.nlm.nih.gov/16834759/

Toepassingen (Applications)

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	p-Chk1 / Chk1 / p-CDK1/2 / CDK1/2 / p-H1		24413181
Growth inhibition assay	Cell viability		31118677

Informatie klinische proef (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2026-05-01)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT06410248	RECRUITING	Recurrent Glioblastoma, IDH-Wildtype; Recurrent WHO Grade 2 Glioma; Recurrent WHO Grade 3 Glioma; Recurrent WHO Grade 4 Glioma	Northwestern University	2024-07-23	PHASE1
NCT06860594	RECRUITING	Astrocytoma, IDH-Mutant, Grade 2; Recurrent Adult Diffuse Hemispheric Glioma, H3 G34-Mutant; Recurrent Adult Diffuse Midline Glioma, H3 K27-Mutant; Recurrent Astrocytoma, IDH-Mutant; Recurrent Astrocytoma, IDH-Mutant, Grade 3; Recurrent Astrocytoma, IDH-Mutant, Grade 4; Recurrent Glioblastoma, IDH-Wildtype	National Cancer Institute (NCI)	2025-07-30	PHASE1
NCT05724108	ACTIVE_NOT_RECRUITING	Metastatic Neuroendocrine Tumor	National Cancer Institute (NCI)	2023-08-30	PHASE2
NCT04494113	ACTIVE_NOT_RECRUITING	Endometrial Serous Adenocarcinoma	National Cancer Institute (NCI)	2022-02-08	EARLY_PHASE1
NCT04234568	ACTIVE_NOT_RECRUITING	Metastatic Digestive System Neuroendocrine Neoplasm; Metastatic Neuroendocrine Tumor	National Cancer Institute (NCI)	2020-07-20	PHASE1
NCT02595879	ACTIVE_NOT_RECRUITING	Advanced Cervical Adenocarcinoma; Advanced Cervical Adenosquamous Carcinoma; Advanced Cervical Squamous Cell Carcinoma; Advanced Vaginal Adenocarcinoma; Advanced Vaginal Adenosquamous Carcinoma; Advanced Vaginal Squamous Cell Carcinoma; Stage IB2 Cervical Cancer AJCC v6 and v7; Stage II Cervical Cancer AJCC v7; Stage II Vaginal Cancer AJCC v6 and v7; Stage III Vaginal Cancer AJCC v6 and v7; Stage IIIB Cervical Cancer AJCC v6 and v7; Stage IVA Cervical Cancer AJCC v6 and v7; Stage IVA Vaginal Cancer AJCC v6 and v7	National Cancer Institute (NCI)	2019-09-18	PHASE1

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Triapine (3-AP) DNA/RNA Synthesis Remmer

Moleculair gewicht: 195.24

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie klinische proef (Clinical Trial Information)

Triapine (3-AP) DNA/RNA Synthesis Remmer

Moleculair gewicht: 195.24

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie klinische proef (Clinical Trial Information)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)