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CSF1R-IN-1 is a CSF1R inhibitor with an with an IC50 of 0.5 nM.

CSF1R is thought to play an important role in recruitment and differentiation of tumor-associated macrophages (TAMs). CSF1R-IN-1 (compound 22) shows good intestinal permeability in a Caco2 assay[1].

CSF1R-IN-1 has favorable pharmacokinetics when dosed orally to mice. It appears suitable for in vivo pharmacology testing in the appropriate preclinical tumor model to demonstrate proof of concept.[1].|| Animal Model:|Male CD-1 mice, 25-35 grams (8-11 weeks old)[1]|Dosage:|2 mg/kg IV or 10 mg/kg orally (Per Os)|Administration:|i.v. or oral|Result:|

[1]. Ramachandran SA, et al. Design, synthesis and optimization of bis-amide derivatives as CSF1R inhibitors. Bioorg Med Chem Lett. 2017 May 15;27(10):2153-2160.

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