sotuletinib

Sotuletinib (BLZ945) is an orally active, effective and specific CSF-1R inhibitor (IC50: 1 nM), >1000-fold selective against its closest receptor tyrosine kinase homologs.

Sotuletinib hydrochloride (BLZ945 HCl) is a selective, brain-penetrant CSF-1R (c-Fms) inhibitor (IC50=1 nM), exhibiting 1000-fold greater selectivity than other receptor tyrosine kinase homologues. It elevates liver enzymes and induces Kupffer cell depletion, making it suitable for studying amyotrophic lateral sclerosis (ALS) and metastatic triple-negative breast cancer (TNBC).

Sotuletinib (BLZ945) dihydrochloride is an orally administered, blood-brain barrier-permeable CSF1-R inhibitor with an IC50 of 1 nM, promoting apoptosis in tumor cells and significantly restricting tumor growth in murine models, thereby proving useful in cancer and amyotrophic lateral sclerosis (ALS) studies [1].