2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  3. c-Fms Akt PERK Aminotransferases (Transaminases) Apoptosis TNF Receptor Interleukin Related
  4. CSF1R-IN-27

CSF1R-IN-27 is a CSF1R inhibitor with oral effectiveness, kinome-wide selective profile, low cellular cytotoxicity, and CSF1R IC50 values of 19 nM, 88 nM, 173 nM, 797 nM, 1448 nM, and >3000 nM. CSF1R-IN-27 suppresses M-CSF-induced phosphorylation of CSF1R, AKT, and ERK in macrophages, and inhibits hepatic p-CSF1R/p-AKT/p-ERK signaling. CSF1R-IN-27 reduces serum transaminase levels, improves hepatic histopathology, alleviates inflammatory cell infiltration, and decreases circulating TNF-α and IL-6 levels. CSF1R-IN-27 can be used for the research of acute liver injury.

For research use only. We do not sell to patients.

CSF1R-IN-27

CSF1R-IN-27 Chemical Structure

CAS No. : 3034296-91-5

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CSF1R-IN-27 Related Antibodies

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Description

CSF1R-IN-27 is a CSF1R inhibitor with oral effectiveness, kinome-wide selective profile, low cellular cytotoxicity, and CSF1R IC50 values of 19 nM, 88 nM, 173 nM, 797 nM, 1448 nM, and >3000 nM. CSF1R-IN-27 suppresses M-CSF-induced phosphorylation of CSF1R, AKT, and ERK in macrophages, and inhibits hepatic p-CSF1R/p-AKT/p-ERK signaling. CSF1R-IN-27 reduces serum transaminase levels, improves hepatic histopathology, alleviates inflammatory cell infiltration, and decreases circulating TNF-α and IL-6 levels. CSF1R-IN-27 can be used for the research of acute liver injury[1].

IC50 & Target[1]

IL-6

 

TNF-α

 

In Vitro

CSF1R-IN-27 (C52) potently inhibits the proliferation of BaF3-ETV6-CSF1R cells at 72 h, with an IC50 value of 0.298 μM[1].
CSF1R-IN-27 (72 h) exhibits low cytotoxicity in H9C2, HUVEC and HepG2 cells, and moderate cytotoxicity in HEK293 and LX-2 cells, with CC50 values ranging from 15.25 μM to >40 μM across all tested cell lines[1].
CSF1R-IN-27 (16-2000 nM; 4 h pretreatment, 30 min M-CSF stimulation) inhibits M-CSF-induced phosphorylation of CSF1R, AKT and ERK in a concentration-dependent manner in RAW264.7 cells and bone marrow-derived macrophages (BMDMs)[1].
CSF1R-IN-27 (24 h) exhibits lower cytotoxicity than PLX3397 in RAW264.7 cells, with a CC50 of 34.70 μM after 24 h of exposure[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CSF1R-IN-27 Related Antibodies

Western Blot Analysis[1]

Cell Line: RAW264.7, bone marrow-derived macrophages (BMDMs)
Concentration: 0, 16, 80, 400, 2000 nM
Incubation Time: 4 h (pretreatment); 30 min (M-CSF stimulation)
Result: Induced concentration-dependent suppression of M-CSF-induced phosphorylation of CSF1R, AKT, and ERK in both RAW264.7 cells and BMDMs.
At concentrations ≥400 nM, substantially attenuated p-CSF1R, p-AKT, and p-ERK levels, with inhibitory effects approaching those of PLX3397 at 400 nM.
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 Vz CL AUC0-t Bioavailability
Mice[1] 10 mg/kg p.o. 1612 μg/L 0.08 h 3.99 h 43.56 L/kg 7.91 L/h/kg 1312 h·μg/L 37 %
Mice[1] 10 mg/kg i.v. 7943 μg/L 0.08 h 4.55 h 19.92 L/kg 2.94 L/h/kg 3499 h·μg/L /
Mice[1] 10 mg/kg i.p. 3613 μg/L 0.21 h 4.45 h 17.45 L/kg 2.91 L/h/kg 3515 h·μg/L /
In Vivo

CSF1R-IN-27 (10-20 mg/kg; p.o.; single administration) exerts dose-dependent hepatoprotective effects against Acetaminophen (HY-66005)-induced acute liver injury in male C57BL/6 mice. Specifically, the oral dose of 20 mg/kg shows superior efficacy to the 10 mg/kg dose in reducing serum transaminase levels, pro-inflammatory cytokine levels, hepatic necrosis, macrophage infiltration, apoptosis, and CSF1R pathway activation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 8 weeks old, 20-25 g, acetaminophen-induced acute liver injury)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: p.o.; single dose
Result: Dose-dependently reduced serum ALT and AST levels compared to the acetaminophen-only model group.
Reduced serum TNF-α and IL-6 levels, with the 20 mg/kg dose showing a more pronounced effect.
Dose-dependently reduced the necrotic area in liver tissue, with the 20 mg/kg dose yielding a greater reduction than the 10 mg/kg dose.
Dose-dependently suppressed hepatic infiltration of CD11b+ and F4/80+ inflammatory macrophages, and reduced the number of TUNEL-positive apoptotic hepatocytes.
Dose-dependently decreased hepatic levels of p-CSF1R, p-AKT, and p-ERK.
Molecular Weight

557.57

Formula

C27H30F3N7O3
CAS No.
SMILES

O=C(N1CCN(C2=CC=C(NC3=NC=CC(OC4=CC=C(NC(C(C)C)=O)C=C4)=N3)C=C2C(F)(F)F)CC1)NC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CSF1R-IN-27 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CSF1R-IN-273034296-91-5c-FmsAktPERKAminotransferases (Transaminases)ApoptosisTNF ReceptorInterleukin RelatedCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RPKBProtein kinase BProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseAminotransferases (Transaminases) Tumor Necrosis Factor ReceptorTNFRILERKH9C2BMDMsBaF3-ETV6-CSF1R cellsmacrophagesHepG2AKTHUVECRAW264.7 cellsInhibitorinhibitorinhibit

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