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CSF1R-IN-1

  Cat. No.:  DC20089   Featured
Chemical Structure
2095849-04-8
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More than 5000 active chemicals with high quality for research!
Field of application
CSF1R-IN-22 is a potent, cellular active and orally bioavailable CSF1R inhibitor with IC50 of 0.5 nM, displays 120-fold selectivity over c-Kit; has improved metabolic stability and Caco2 permeability.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
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.
MSDS
COA
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2018-0101
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