Sotuletinib (dihydrochloride)

Sotuletinib (BLZ945) dihydrochloride is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC₅₀ of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib dihydrochloride can be used for microglia depletion, and for tumor and CNS-related disease research^[1][2][3][4]. IC50 & Target:IC50: CSF1-R (1 nM)^[1]. In Vivo:Sotuletinib (2,000 ppm in diet, 21 days) dihydrochloride depletes more than 90% of microglia in C57BL6/J mice^[3].
Sotuletinib hydrochloride (200 mg/kg, p.o., 7 days) depletes more than 90% microglia in C57BL6/J mice, and subsequntenly used for microglia replacement^[4].
Sotuletinib (60-169 mg/kg, p.o., 5 days) dihydrochloride dose- and time-dependently depletes microglia in C57BL6/J mice, and newly generated microglia after BLZ945 removal reached normal levels 3 days after last dose^[5].