PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor with an Ki of 5.9 nM. PLX5622 eliminates microglia from the brain, which can be sustained in wild-type and the Alzheimer's disease model mice (3xTg-AD model). In the AD model PLX5622 prevents microglial association with amyloid β plaques and improves cognition.
In vivo, PLX5622 (65 mg/kg/day; oral gavage for 14 days) causes paw withdrawal threshold high in mice, indicating that PLX5622 prevents the development of injury-associated mechanical allodynia.
| Molecular Weight | 395.41 |
| Formula | C21H19F2N5O |
| CAS Number | 1303420-67-8 |
| Solubility (25°C) | DMSO ≥ 65 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. |
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