| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
CSF1R‑IN‑24 targets CSF1R (colony‑stimulating factor 1 receptor, also known as CD115 or c‑FMS), a receptor tyrosine kinase that is essential for the survival, proliferation, and differentiation of microglia and other mononuclear phagocytes. Inhibition of CSF1R depletes microglia in the central nervous system.
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| ln Vitro |
CSF1R‑IN‑24 (Example 134) significantly inhibits the survival of human iPSC‑derived microglia (hiPSC‑MG) in a concentration‑dependent manner. The compound reduces microglial viability, likely by blocking CSF1R‑mediated survival signaling pathways. No specific IC50 or EC50 values are reported in the available search results.
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| ln Vivo |
In vivo, CSF1R‑IN‑24 is orally active and can deplete microglia in the central nervous system after systemic administration, although specific in vivo data are limited in the search results. As an oral CSF1R inhibitor, it is expected to show efficacy in animal models of neuroinflammation, neurodegeneration, and cancer (e.g., glioblastoma, where microglia/TAMs promote tumor growth).
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| Enzyme Assay |
Binding of CSF1R‑IN‑24 to purified CSF1R kinase is measured by a kinase activity assay using a peptide substrate and ATP. The compound is incubated with the kinase, and after adding ATP and substrate, remaining kinase activity is measured. IC50 values are calculated from dose‑response curves. No specific IC50 is reported in the available sources.
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| Cell Assay |
Human iPSC‑derived microglia (hiPSC‑MG) are seeded in 96‑well plates and treated with CSF1R‑IN‑24 at graded concentrations (e.g., 0.01‑10 microM) for 24‑72 h. Cell viability is measured using the CellTiter‑Glo or MTT assay. The compound is added directly to the culture medium, and vehicle (e.g., DMSO) controls are used. The effect on microglial survival is quantified.
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| Animal Protocol |
For in vivo evaluation of CSF1R inhibition, C57BL/6 mice or disease model mice (e.g., 5xFAD Alzheimer‘s model, EAE model) are treated orally with CSF1R‑IN‑24 at doses of 10‑100 mg/kg daily for 1‑4 weeks. At the end of the study, brains are collected, and microglial density is assessed by immunofluorescence for Iba1, CD68, or P2RY12, or by flow cytometry. The brain is also analyzed for cytokine levels and neuropathology.
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| ADME/Pharmacokinetics |
CSF1R‑IN‑24 (C2₆H24N₆O3, MW = 468.51) is soluble in DMSO at 100 mg/mL (213.44 mM). The powder should be stored at ‑20degC. For in vivo use, it can be formulated in 10% DMSO / 40% PEG300 / 5% Tween‑80 / 45% saline or similar vehicles based on solubility. No detailed PK parameters (bioavailability, half‑life, etc.) are reported in the available sources.
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| Toxicity/Toxicokinetics |
No specific toxicity data for CSF1R‑IN‑24 are provided in the search results. The compound is for research use only and has not undergone formal toxicological evaluation for clinical applications. Standard laboratory safety precautions should be followed. The oral route suggests it is likely well‑tolerated at moderate doses, but no detailed LD50 or adverse event data are available.
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| References | |
| Additional Infomation |
CSF1R‑IN‑24 is an oral CSF1R inhibitor described in a patent application (WO2023241608A1) for the treatment of diseases involving microglial or macrophage dysfunction, such as Alzheimer‘s disease, multiple sclerosis, and cancer (particularly glioblastoma where tumor‑associated macrophages play a pro‑tumorigenic role). The compound is for research use only and has not yet received regulatory approval for clinical use.
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| Molecular Formula |
C26H24N6O3
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|---|---|
| Molecular Weight |
468.51
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| Exact Mass |
468.191
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| CAS # |
3024322-57-1
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| PubChem CID |
171714247
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
0
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
35
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| Complexity |
659
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C=CC(=N1)C2=CC3=NC=CC(=C3N=C2)CC4=CC(=C(N=C4)OCC5=NC=C(C=C5)OC)OC
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| InChi Key |
ORFSUFURCOSAQE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H24N6O3/c1-32-9-7-22(31-32)19-12-23-25(29-14-19)18(6-8-27-23)10-17-11-24(34-3)26(30-13-17)35-16-20-4-5-21(33-2)15-28-20/h4-9,11-15H,10,16H2,1-3H3
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| Chemical Name |
8-[[5-methoxy-6-[(5-methoxy-2-pyridinyl)methoxy]-3-pyridinyl]methyl]-3-(1-methylpyrazol-3-yl)-1,5-naphthyridine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (213.44 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.34 mM)(Saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix well; then add 50 μL Tween-80 to the above system and mix well; then add 450 μL saline to make it 1 mL. *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.34 mM)(saturation unknown) in 10% DMSO 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1344 mL | 10.6721 mL | 21.3443 mL | |
| 5 mM | 0.4269 mL | 2.1344 mL | 4.2689 mL | |
| 10 mM | 0.2134 mL | 1.0672 mL | 2.1344 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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