CSF1R/c-Kit-IN-2

CSF1R/c-Kit-IN-2 (11o) (40 min) potently inhibits recombinant human CSF-1R with an IC₅₀ of 6.84 nM^[1].
CSF1R/c-Kit-IN-2 (40 min) potently inhibits recombinant human c-Kit with an IC₅₀ of 0.95 nM, exhibiting stronger activity against c-Kit than CSF-1R^[1].
CSF1R/c-Kit-IN-2 (1.0 μM; 20 min pre-incubation, 2 h incubation) exhibits off-target activity against FYN, ABL1, and CSK with IC₅₀ values of 11.4 nM, 14.2 nM, and 118 nM, respectively, while remaining most potent against c-Kit and CSF-1R^[1].
CSF1R/c-Kit-IN-2 (10 μM; 6 h) does not reduce SIM-A9 mouse microglial cell viability when treated at 10 μM for 6 h^[1].
CSF1R/c-Kit-IN-2 (1-10 μM; 30 min pretreatment, 20 min CSF-1 stimulation) suppresses CSF-1-induced ERK phosphorylation in SIM-A9 mouse microglial cells in a concentration-dependent manner, reducing residual pERK/total ERK to 21.9% at 10 μM^[1].
CSF1R/c-Kit-IN-2 (30 min) shows high human liver microsomal stability, with 86.2% of the compound remaining after 30 min incubation at 37°C^[1].
CSF1R/c-Kit-IN-2 exhibits favorable blood-brain barrier permeability with an effective permeability coefficient (P_e) of 16.97 × 10^-6 cm/s^[1].
CSF1R/c-Kit-IN-2 (60 min) exhibits excellent human plasma stability, with >100% of the compound remaining after 60 min incubation at room temperature^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.