CSF1R-IN-1 is a CSF1R inhibitor with an with an IC 50 of 0.5 nM.
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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. . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CD-1 mice, 25-35 grams (8-11 weeks old) Dosage: 2 mg/kg IV or 10 mg/kg orally (Per Os) Administration: i.v. or oral Result: I.V.: C max =3.55, T 1/2 =0.87\nP.O.: C max =4.6, T 1/2 =1.8, Bioavailability=64%
