alleen voor onderzoeksdoeleinden
Cat.nr.: S1305
Chemische structuur
| Gerelateerde doelwitten | HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF |
|---|---|
| Overig DNA/RNA Synthesis Inhibitoren | CX-5461 (Pidnarulex) SCR7 Favipiravir (T-705) RK-33 EED226 BMH-21 Carmofur Triapine (3-AP) YK-4-279 Halofuginone |
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| L1210 leukemia cells | Function assay | Inhibitory concentration on multidrug-resistant L1210 leukemia cells, IC50=0.024 μM | ||||
| MT4 cells | Proliferation assay | Antiproliferative activity against human MT4 cells by MTT assay, IC50=0.1 μM | ||||
| human CCRF-CEM cells | Proliferation assay | Antiproliferative activity against human CCRF-CEM cells by MTT assay, IC50=1 μM | ||||
| human CCRF-SB cells | Proliferation assay | Antiproliferative activity against human CCRF-SB cells by MTT assay, IC50=1 μM | ||||
| human SK-MEL-28 cells | Proliferation assay | Antiproliferative activity against human SK-MEL-28 cells by MTT assay, IC50=15 μM | ||||
| human MCF7 cells | Proliferation assay | Antiproliferative activity against human MCF7 cells by MTT assay, IC50=3 μM | ||||
| human HepG2 cells | Proliferation assay | Antiproliferative activity against human HepG2 cells by MTT assay, IC50=8 μM | ||||
| human DU145 cells | Proliferation assay | Antiproliferative activity against human DU145 cells by MTT assay, IC50=2 μM | ||||
| mouse J774.A1 cells | Proliferation assay | 3 days | Antiproliferative activity against mouse J774.A1 cells after 3 days by MTT conversion assay, IC50=0.003 μM | |||
| HEK293 cells | Proliferation assay | 3 days | Antiproliferative activity against HEK293 cells after 3 days by MTT conversion assay, IC50=0.007 μM | |||
| mouse J774 cells | Proliferation assay | 72 h | Antiproliferative activity against mouse J774 cells assessed as reduction of cell growth after 72 hrs by MTT method, IC50=0.003 μM | |||
| human PBMC | Function assay | 4 days | Inhibition of T cell mitogen-induced blastogenesis in human PBMC after 4 days, IC50=0.1495 μM | |||
| HeLa cells | Cytotoxicity assay | 48 h | Cytotoxicity against human HeLa cells at lag phase of growth after 48 hrs by MTT assay, IC50=2.9 μM | |||
| A549 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human A549 cells at lag phase of growth after 48 hrs by MTT assay, IC50=47 μM | |||
| MCF7 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human MCF7 cells at lag phase of growth after 48 hrs by MTT assay, IC50=1.4 μM | |||
| MT4 cells | Cytotoxicity assay | 96 h | Cytotoxicity against human MT4 cells infected with HTLV-1 after 96 hrs by MTT assay, CC50=0.1 μM | |||
| CCRF-CEM cells | Proliferation assay | 96 h | Antiproliferative activity against human CCRF-CEM cells after 96 hrs by MTT assay, CC50=1 μM | |||
| WIL2-NS cells | Proliferation assay | 96 h | Antiproliferative activity against human WIL2-NS cells after 96 hrs by MTT assay, CC50=3 μM | |||
| CCRF-SB cells | Proliferation assay | 96 h | Antiproliferative activity against human CCRF-SB cells after 96 hrs by MTT assay, CC50=1.1 μM | |||
| human DU145 cells | Proliferation assay | 96 h | Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay, CC50=2 μM | |||
| human HepG2 cells | Proliferation assay | 96 h | Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay, CC50=8 μM | |||
| MCF7 cells | Proliferation assay | 96 h | Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay, CC50=3.2 μM | |||
| SK-MEL-28 cells | Proliferation assay | 96 h | Antiproliferative activity against human SK-MEL-28 cells after 96 hrs by MTT assay, CC50=15 μM | |||
| MCF7 cells | Cytotoxicity assay | Cytotoxicity against human MCF7 cells, IC50=2.79 μM | ||||
| mouse S49 cells | Cytotoxicity assay | 72 h | Cytotoxicity against wild type mouse S49 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay, EC50=8 μM | |||
| Colo-357 cells | Cytotoxicity assay | Cytotoxicity against human Colo-357 cells by crystal violet staining, IC50=6.12 μM | ||||
| Aspc-1 cells | Cytotoxicity assay | Cytotoxicity against human Aspc-1 cells by crystal violet staining, IC50=2.45 μM | ||||
| A549 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay, IC50=47 μM | |||
| MCF7 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay, IC50=1.4 μM | |||
| Patu-02 cells | Cytotoxicity assay | Cytotoxicity against human Patu-02 cells by crystal violet staining, IC50=9.69 μM | ||||
| Patu-T cells | Cytotoxicity assay | Cytotoxicity against human Patu-T cells by crystal violet staining, IC50=4.09 μM | ||||
| Patu-S cells | Cytotoxicity assay | Cytotoxicity against human Patu-S cells by crystal violet staining, IC50=11.07 μM | ||||
| T3M4 cells | Cytotoxicity assay | Cytotoxicity against human T3M4 cells by crystal violet staining, IC50=2.63 μM | ||||
| human PANC1 cells | Cytotoxicity assay | Cytotoxicity against human PANC1 cells by crystal violet staining, IC50=6.39 μM | ||||
| human DAN-G cells | Cytotoxicity assay | Cytotoxicity against human DAN-G cells by crystal violet staining, IC50=4.06 μM | ||||
| HeLa cells | Cytotoxicity assay | 48 h | Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay, IC50=2.9 μM | |||
| WEHI164 cells | Proliferation assay | 3 days | Antiproliferative activity against mouse WEHI164 cells after 3 days by MTT conversion assay, IC50=0.015 μM | |||
| WIL-2NS cells | Proliferation assay | Antiproliferative activity against human WIL-2NS cells by MTT assay, IC50=3 μM | ||||
| WEHI164 cells | Proliferation assay | 72 h | Antiproliferative activity against mouse WEHI164 cells assessed as reduction of cell growth after 72 hrs by MTT method, IC50=0.017 μM | |||
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
| Molecuulgewicht | 152.18 | Formule | C5H4N4S |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 50-44-2 | SDF downloaden | Opslag van stamoplossingen |
|
|
| Synoniemen | 6-MP | Smiles | C1=NC2=C(N1)C(=S)N=CN2 | ||
|
In vitro |
DMSO
: 30 mg/mL
(197.13 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)
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 de sectie oplosbaarheid.)
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.
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. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
| Targets/IC50/Ki |
PRPP Amidotransferase
|
|---|---|
| In vitro |
Mercaptopurine (6-MP) is widely used to treat malignancies, rheumatic diseases, dermatologic conditions, inflammatory bowel disease, and solid organ transplant rejection. It inhibits purine nucleotide synthesis and metabolism by inhibiting an enzyme called Phosphoribosyl pyrophosphate amidotransferase (PRPP Amidotransferase). PRPP Amidotransferase is the rate limiting enzyme of purine synthesis. This compound alters the synthesis and function of RNA and DNA. It interferes with nucleotide interconversion and glycoprotein synthesis. |
Referenties |
|
(gegevens van https://clinicaltrials.gov, bijgewerkt op 2026-07-30)
| NCT-nummer | Werving | Aandoeningen | Sponsor/medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| NCT07072585 | NOT_YET_RECRUITING | Stage II T Lymphoblastic Leukemia/Lymphoma; Stage III T Lymphoblastic Leukemia/Lymphoma; Stage IV T Lymphoblastic Leukemia/Lymphoma; T Acute Lymphoblastic Leukemia; T Lymphoblastic Lymphoma |
Children's Oncology Group |
2026-08-28 | PHASE2; PHASE3 |
| NCT07716735 | NOT_YET_RECRUITING | Advanced Kidney Carcinoma; Advanced Renal Cell Carcinoma; Hereditary Leiomyomatosis and Renal Cell Carcinoma; Metastatic Kidney Carcinoma; Metastatic Renal Cell Carcinoma; Skin Leiomyoma; Stage III Renal Cell Cancer AJCC v8; Stage IV Renal Cell Cancer AJCC v8; Uterine Corpus Leiomyoma |
Jonsson Comprehensive Cancer Center |
2026-12-01 | PHASE1 |
| NCT06099366 | RECRUITING | Lymphoblastic Leukemia in Children |
Hee Young Ju |
2024-03-05 | PHASE2 |
| NCT03959085 | RECRUITING | B Acute Lymphoblastic Leukemia; B Lymphoblastic Lymphoma; Central Nervous System Leukemia; Mixed Phenotype Acute Leukemia; Testicular Leukemia |
Children's Oncology Group |
2019-10-31 | PHASE3 |
| NCT07636564 | NOT_YET_RECRUITING | Acute Leukemia of Ambiguous Lineage; B Acute Lymphoblastic Leukemia; B Acute Lymphoblastic Leukemia, Philadelphia Chromosome Negative; T Acute Lymphoblastic Leukemia |
SWOG Cancer Research Network |
2026-10-14 | PHASE2 |
| NCT07431060 | RECRUITING | Langerhans Cell Histiocytosis (LCH) |
West China Second University Hospital |
2026-02-13 |