CSF1R-IN-22( —— )

Catalog No. M13301 CAS No. 2095849-04-8

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

CSF1R-IN-22
Note

Research use only, not for human use.
Brief Description

CSF1R-IN-22 is a potent, cellular active and orally bioavailable CSF1R inhibitor with IC50 of 0.5 nM.
Description

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.
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.
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.. 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%
Synonyms

——
Pathway

Tyrosine Kinase
Target

CSF1R
Recptor

CSF1R
Research Area

——
Indication

——

CAS Number

2095849-04-8
Formula Weight

479.463
Molecular Formula

C25H20F3N5O2
Purity

>98% (HPLC)
Solubility

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

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
Chemical Name

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

1. Ramachandran SA, et al. Bioorg Med Chem Lett. 2017 May 15;27(10):2153-2160.

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