CSF1R-IN-15
CSF1R-IN-15 (compound 23) is an inhibitor targeting CSF1R. The colony-stimulating factor-1 receptor (CSF1R) is a tyrosine kinase embedded in the cell membrane of macrophages. The receptor is activated by colony-stimulating factor-1 (CSF-1) and interleukin-34, and signaling via CSF1R is crucial for the differentiation, proliferation, and survival of macrophages.
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- CAS No.: 2925744-43-8
- 화학식: C22H22N4O
- 분자량:358.44
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
>9.9 μM
Compound: 27g
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Cytotoxicity against IL-3-dependent mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay
Cytotoxicity against IL-3-dependent mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay
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[PMID: 38141285] |
CSF1R-IN-15 (0.007-10 μM, 72 h) is inactive to Ba/F3 cell viability, while Pex significantly (HY-16749) showed superior activity [1].
CSF1R-IN-15 assessment of plasma protein binding is measured by equilibrium dialysis. CSF1R-IN-15 (5 μM, 6 h, 37 °C) was incubated with plasma and showed 69% binding to mouse plasma proteins[1].
Pharmacokinetic Analysis for CSF1R-IN-15 (compound 23) in vitro[1]
| HLM CLint(μL/min/mg) | HLM CLint(μL/min/mg) | HLM CLint(μL/min/mg) | Plasmastab. | PPB |
| 15.5 | 40 | 86 | 69 | 94 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3-hCSF1R Cells
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Concentration:0.007-10 μM
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Incubation Time:72 h
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Result:Exhibited no activity while pexidartinib (HY-16749) has superior activity.
Pharmacokinetic Analysis in CSF1R-IN-15 (compound 23) for a cassette dosing study in C57BLKS mice[1]
| t1/2 (h) | C0 (ng/mL) | AUC0-∞ (h*ng/mL) | CLobs (L/h/kg) | Vss,obs (L/kg) |
| 0.5 | 37 | 18 | 54 | 32 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:In Vivo Pharmacokinetic Study
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Dosage:1mg/kg
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Administration:Intravenous injection (i.v.) single dosing of drugs (1 mg/kg each) in a 20% DMSO, 80% PEG400 formulation. Blood sampling was done after 10, 30, 60, 120, 240, and 480 min.
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Result:In vivo pharmacokinetic indexes were t1/2 (0.5 h), C0 (37 ng/mL), AUC0-∞ (18 h*ng/mL), CLobs (54 L/h/kg), and Vss,obs (32 L/kg), respectively.
Chemical Information
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CAS No. 2925744-43-8
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분자량 358.44
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화학식 C22H22N4O
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SMILES
CN(C1=NC=NC2=C1C=C(N2)C3=CC=C(C=C3)CO)CC4=CC=CC(C)=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CSF1R-IN-15 Related Classifications
HY-155001 Related Classifications
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