ICT12035
ICT12035 (AZ2158) is a selective small-molecule FPR1 antagonist with an IC50 of 30 nM. ICT12035 reduces fMLF-induced proliferation and invasion and modulates xenograft tumor growth. ICT12035 is used in research on glioblastoma, bladder cancer, and glioma.
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- CAS No.: 1355994-75-0
- Formule: C25H38N4O4S
- Masse moléculaire:490.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
FPR1 30 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-87MG ATCC | IC50 |
30 nM
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Antagonism of FPR1 receptor activation by 100 nM fMLF in U87-MG glioblastoma cells assessed by calcium mobilisation (flux) assay using Fluo-4 NW dye.
Antagonism of FPR1 receptor activation by 100 nM fMLF in U87-MG glioblastoma cells assessed by calcium mobilisation (flux) assay using Fluo-4 NW dye.
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33057069 |
In Vitro
ICT12035 (AZ2158) (1 µM) blocked fMLF-induced calcium mobilization in PC-3, SH-SY-5Y, and HCT-116 cancer cells[1].
ICT12035 (100 µM; 96 h) showed no cytotoxicity against U87-MG cells, with cell viability above 95% at 100 µM[1].
ICT12035 (1 µM; 5 days) eliminated the fMLF-induced increase in U87-MG cell proliferation in 2D culture[1].
ICT12035 (1 µM; treated once every 24 h; monitored at 146 h, 172 h, and 197 h for up to 9 days) delayed the fMLF-induced increase in U87-MG multicellular spheroid growth[1].
ICT12035 (2-20 µM; analyzed at 18 h and 39 h) eliminated the fMLF-induced increase in invasion of U87-MG multicellular spheroids[1].
ICT12035 (10 nM-100 µM; 16 h) reduced the fMLF-induced increase in U87-MG cell invasion in a dose-dependent manner[1].
ICT12035 (30 min) is a potent antagonist of FPR1 in U87-MG cells, with an IC50 of 30 nM[1] in calcium mobilization assays.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87-MG
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Concentration:100 µM
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Incubation Time:96 h (incubation); 4 h (MTT)
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Result:Showed cell viability above 95% at 100 µM.
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Cell Line:U87-MG
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Concentration:1 µM
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Incubation Time:5 days
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Result:Abrogated the fMLF-induced increase in cell numbers.
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Cell Line:U87-MG multicellular spheroids
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Concentration:2 µM and 20 µM
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Incubation Time:Analyzed at 18 h and 39 h
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Result:Abrogated the fMLF-induced increase in cross-section area, with significant reductions at 2 µM and 20 µM.
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Cell Line:U87-MG
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Concentration:10 nM, 100 nM, 1 µM, 10 µM and 100 µM
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Incubation Time:16 h
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Result:Retarded the invasion of U87-MG cells in a dose-dependent manner.
Significant reductions in migrated cells were observed at 10 nM, 100 nM, 1 µM, 10 µM and 100 µM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c immunodeficient nude mice (6-8 weeks old)[1]
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Dosage:100 mg/kg
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Administration:i.p.; days 0, 1, 2, 3 and 4
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Result:Completely arrested tumor growth during the 5-day treatment period.
Increased median time to reach a relative tumor volume of 2 (RTV2) to 15.5 days versus 9.4 days for untreated controls, corresponding to a six day delay in further growth.
No signs of toxicity were evident.
- Patient-Derived Xenograft (PDX)
- Patient-Derived Orthotopic Xenograft (PDOX)
- Cell invasion
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 1355994-75-0
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Masse moléculaire 490.66
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Formule C25H38N4O4S
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SMILES
O=S(NC1=C(C(N[C@@H](C)C(C)(C)C)=O)C(C)=NN1[C@@H]2CC[C@@H](CC2)OC)(C3=CC=C(C=C3)C)=O
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Synonyms
AZ2158
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)