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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3034296-91-5
- Formule: C27H30F3N7O3
- Masse moléculaire:557.57
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform TNF Receptor
More
Activité biologique
|
IL-6 |
TNF-α |
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.
-
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.
| 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 | / |
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.
Chemical Information
-
CAS No. 3034296-91-5
-
Masse moléculaire 557.57
-
Formule C27H30F3N7O3
-
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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz