| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| Other Sizes |
| Targets |
CSF1R-IN-3 targets the colony-stimulating factor 1 receptor (CSF-1R), also known as c-Fms. CSF-1R is a receptor tyrosine kinase that plays a key role in the survival, proliferation, and differentiation of macrophages. Inhibition of CSF-1R suppresses tumor-associated macrophages (TAMs) and modulates the tumor immune microenvironment.
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| ln Vitro |
In vitro, CSF1R-IN-3 is a potent CSF-1R inhibitor with an IC₅₀ of 2.1 nM. It has anti-proliferative activity against colorectal cancer cells. It inhibits the progression of colorectal cancer by suppressing the migration of macrophages and reprograming M2-like macrophages to the M1 phenotype.
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| ln Vivo |
In vivo, CSF1R-IN-3 is orally effective. It exhibits antitumor effects and enhances immunity by inhibiting macrophage migration and reprogramming M2-like macrophages to the M1 phenotype. It has potential for cancer immunotherapy research.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for CSF1R-IN-3 involves measuring the kinase activity of CSF-1R in the presence of the compound. The IC₅₀ of 2.1 nM is determined by quantifying the reduction in CSF-1R-mediated phosphorylation.
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| Cell Assay |
In vitro cell-based assays for CSF1R-IN-3 involve treating colorectal cancer cells or macrophages with the compound and assessing cell viability, proliferation, and macrophage polarization. The compound's effects on macrophage migration and phenotype are evaluated.
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| Animal Protocol |
In vivo animal studies for CSF1R-IN-3 would likely involve xenograft mouse models of colorectal cancer. Tumor-bearing mice would be treated orally with the compound, and tumor growth inhibition would be monitored. The compound's effects on tumor-associated macrophages and antitumor immunity would be assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CSF1R-IN-3 are not extensively detailed in the available literature. The compound is orally effective.
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| Toxicity/Toxicokinetics |
No specific toxicity data for CSF1R-IN-3 are available in the provided literature. The compound is for research use only. Standard laboratory safety precautions should be followed when handling.
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| References | |
| Additional Infomation |
CSF1R-IN-3 is an orally effective CSF-1R inhibitor with an IC₅₀ of 2.1 nM. It has anti-proliferative activity against colorectal cancer cells. It enhances antitumor immunity. Its CAS number is 2760584-90-3.
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| Molecular Formula |
C30H38N8O4
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|---|---|
| Molecular Weight |
574.673925876617
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| Exact Mass |
574.301
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| CAS # |
2760584-90-3
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| PubChem CID |
162719835
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| Appearance |
Yellow to orange solid powder
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
42
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| Complexity |
1040
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(CC(NC2C(C)=C(/C=C3/C4=C(NC/3=O)C=C(NC(NC3C=C(C(C)(C)C)ON=3)=O)C=C4)NC=2C)=O)CCN(C)CC1
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| InChi Key |
YLKFFTVAKILRBN-STZFKDTASA-N
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| InChi Code |
InChI=1S/C30H38N8O4/c1-17-22(31-18(2)27(17)35-26(39)16-38-11-9-37(6)10-12-38)14-21-20-8-7-19(13-23(20)33-28(21)40)32-29(41)34-25-15-24(42-36-25)30(3,4)5/h7-8,13-15,31H,9-12,16H2,1-6H3,(H,33,40)(H,35,39)(H2,32,34,36,41)/b21-14-
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| Chemical Name |
N-[5-[(Z)-[6-[(5-tert-butyl-1,2-oxazol-3-yl)carbamoylamino]-2-oxo-1H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrol-3-yl]-2-(4-methylpiperazin-1-yl)acetamide
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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 : ~62.5 mg/mL (~108.76 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7401 mL | 8.7006 mL | 17.4013 mL | |
| 5 mM | 0.3480 mL | 1.7401 mL | 3.4803 mL | |
| 10 mM | 0.1740 mL | 0.8701 mL | 1.7401 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.
Products are for research use only; We do not sell to patients
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