CSF1R-IN-22

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CSF1R-IN-22 是一种有效的、细胞活性的、口服生物可利用的 CSF1R 抑制剂，IC50 为 0.5 nM。

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.

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.

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

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Tyrosine Kinase

CSF1R

CSF1R

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2095849-04-8

479.463

C25H20F3N5O2

>98% (HPLC)

In Vitro:?DMSO : 83.33 mg/mL (173.80 mM)

CC1=CC=C(NC(C2=CC=CC(C(F)(F)F)=C2)=O)C=C1NC(C3=CC(C4=CN(C)N=C4)=CN=C3)=O

5-(1-methyl-1H-pyrazol-4-yl)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)nicotinamide

(-20℃)

With Ice Pack

≥ 2 years