Edicotinib (JNJ-40346527) is a potent, selective, blood-brain permeable and orally active CSF-1R inhibitor.IC50 3.2 nM. Edicotinib has less inhibitory effect on KIT and FLT3,IC50 The values are 20 nM and 190 nM, respectively. Edicotinib inhibits the expansion of microglia, weakens the proliferation of microglia and neurodegenerative degeneration. Edicotinib can be used in the study of Alzheimer's disease and rheumatoid arthritis.
| Molecular Weight | 461.6 |
| Formula | C27H35N5O2 |
| CAS Number | 1142363-52-7 |
| Solubility (25°C) | DMSO ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related CSF-1R (c-Fms) Products |
|---|
| Tinengotinib
Tinengotinib is a modulator of several protein kinases, such as Aurora kinase, VEGFR kinase, and CSF-1R, etc. Tinengotinib can be used in studies related to diseases mediated by abnormalities in these kinases. |
| AMG-820
AMG-820 is an anti-colony stimulating factor 1 receptor (CSF1R) monoclonal antibody. |
| CSF1R-IN-15
CSF1R-IN-15 is an inhibitor targeting CSF1R. |
| Pimicotinib
Pimicotinib is a novel, orally bioavailable, highly selective small-molecule inhibitor of colony-stimulating factor 1 (CSF-1) with antitumor activity and less inhibitory effects on c-Kit and PDGFR. |
| c-Fms-IN-14
c-Fms-IN-14 is a c-Fms inhibitor with an IC50 value of 4 nM. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
