Cas No.: | 2095849-04-8 |
SMILES: | C(NC1=CC(NC(=O)C2=CC=CC(C(F)(F)F)=C2)=CC=C1C)(=O)C1=CN=CC(C2=CN(C)N=C2)=C1 |
Formula: | C25H20F3N5O2 |
M.Wt: | 479.45 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | 1. Ramachandran SA, et al. Bioorg Med Chem Lett. 2017 May 15;27(10):2153-2160. |
Description: | CSF1R-IN-1 is a CSF1R inhibitor with an with an IC50 of 0.5 nM. |
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]. |
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. |