2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.：2095849-04-8 Product Name： Synonyms： EINEC: Molecular Formula：C25H20F3N5O2 Molecular Weight：479.45
Target:
IC50: 0.5 nM (CSF1R)[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%
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].
Kinase Assay
Cell Assay
Animal Administration
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.
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