|Cat. No.||Product Name||CAS No.||Information|
JTE-952 (JTE952) is a potent, selective colony stimulating factor-1 receptor (CSF1R) type II inhibitor with IC50 of 14 nM, shows cellular activity in BMMCs IL-6 secretion assays with IC50 of 20 nM; JTE-952 is also effective against a mouse collagen-induced model of arthritis (mouse CIA-model).
Ki20227 is a potent, selective, orally active c-Fms inhibitor with IC50 of 2 nM; weakly inhibits KDR, c-Kit, and PDGFRβ with IC50 of 12, 451, and 217 nM, respectively, no activty against Flt-3, c-Src, Fyn, EGFR, FGFR2, Met, Btk, PKA, and PKCα (IC50>1,000 nM); inhibits the M-CSF-dependent cell growth, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model.
BLZ945 (BLZ-945) is a potent, selective, brain-penetrant CSF-1R inhibitor with biochemical IC50 of 1 nM, displays >3,200-fold selectivity over other kinases (c-Kit, PDGFR-β, Flt3, Abl, etc.); inhibits CSF-1-dependent proliferation in bone marrow-derived macrophages (BMDMs) with EC50 of 67 nM, and decreases CSF-1R phosphorylation; blocks glioma progression and significantly improves survival, efficiently limits tumor progression combining with PD-1/PD-L1 blocking antibodies in neuroblastoma.
Pexidartinib is an oral-active, BBB-penatrant, potent mutil-targeted RTK inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively; inhibits the CSF1-dependent proliferation with IC50 of 0.44 uM, 0.22 uMand 0.1 uM in M-NFS-60, Bac1.2F5 and M-07e cells, respectively; significantly inhibits PTX-induced tumor infiltration in mice.
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