CSF1R-IN-1

Names

[ CAS No. ]:
2095849-04-8

[ Name ]:
CSF1R-IN-1

Biological Activity

[Description]:

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

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Fms

[Target]

IC50: 0.5 nM (CSF1R)[1]

[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[1].

[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.[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: I.V.: Cmax=3.55, T1/2=0.87P.O.: Cmax=4.6, T1/2=1.8, Bioavailability=64%

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₀F₃N₅O₂

[ Molecular Weight ]:
479.45

Related Compounds

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