1. Protein Tyrosine Kinase/RTK
  2. c-Fms
  3. 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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CSF1R-IN-15 Chemical Structure

CSF1R-IN-15 Chemical Structure

CAS No. : 2925744-43-8

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Description

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[1].

In Vitro

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]

CSF1R-IN-15 (compound 23) 体外药代动力学分析[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.

Cell Viability Assay[1]

Cell Line: Ba/F3-hCSF1R Cells
Concentration: 0.007-10 μM
Incubation Time: 72 h
Result: Exhibited no activity while pexidartinib (HY-16749) has superior activity.
In Vivo

In vivo pharmacokinetic indices were derived from cassette dosing studies. The t1/2, C0, AUC0-∞, CLobs, and Vss,obs of CSF1R-IN-15 were 0.5 h, 37 ng/mL, 18 h*ng/mL, 54 L/h/kg, and 32 L/kg in C57BLKS mice[1].
Pharmacokinetic Analysis in CSF1R-IN-15 (compound 23) for a cassette dosing study in C57BLKS mice[1]

CSF1R-IN-15 (compound 23) 在 C57BLKS 小鼠中的体内药代动力学分析[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.

Animal Model: In Vivo Pharmacokinetic Study
Dosage: 1mg/kg
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.
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.
Molecular Weight

358.44

Formula

C22H22N4O

CAS No.
SMILES

CN(C1=NC=NC2=C1C=C(N2)C3=CC=C(C=C3)CO)CC4=CC=CC(C)=C4

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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References
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CSF1R-IN-15 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CSF1R-IN-15
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HY-155001
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