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You are here:Home-Inhibitors & Agonists-Tyrosine Kinase-c-Fms (CSF1R)

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Colony stimulating factor 1 receptor (CSF1R, c-Fms, CD115) is a tyrosine kinase transmembrane receptor for a cytokine called colony stimulating factor 1 (CSF-1). CSF-1R and its ligands, CSF-1 and interleukin 34 (IL-34), regulate the function and survival of tumor-associated macrophages, which are involved in tumorigenesis and in the suppression of antitumor immunity. In solid tumors, targeting CSF-1R via either small molecules or antibodies has shown interesting results in vitro but limited antitumor activity in vivo. Blocking CSF-1/CSF-1R signaling represents a promising immunotherapy approach and several new potential combination therapies for future clinical testing. PLX-3397 (pexidartinib) is an oral, potent, multi-target receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 and is the most advanced selective CSF-1R inhibitor under clinical development. ABT-869 (linifanib) is an oral inhibitor of CSF-1R tyrosine kinase conducted a phase II trial in which ABT869 was administered to patients with hepatocellular carcinoma. BLZ-945 is another orally active, bioavailable, potent, and selective inhibitor of CSF-1R, which is currently being assessed in a first-in-man phase I/II study as a single agent or in combination with PDR-001 (anti-PD-1 antibody) in several advanced solid tumors. Besides, multiple anti-CSF-1R monoclonal antibodies have also entered clinical trials, including FPA-008 (cabiralizumab), RG-7155 (RO5509554), IMC-CS4 (LY3022855) and AMG-820. The development of new CSF-1R/CSF-1 axis inhibitors represents an attractive method for managing patients with metastatic solid tumors refractory to the standards of care or with diffuse/relapsed TGCT. Recent clinical trials testing CSF-1R inhibitors as monotherapies have shown encouraging results in the management of PVNS but disappointing outcomes for the treatment of solid tumors. References: 1. Peyraud F, et al. Curr Oncol Rep. 2017 Sep 5;19(11):70. 2. Pyonteck SM, et al. Nat Med. 2013 Oct;19(10):1264-72. 3. Kogan M, et al. Anticancer Res. 2012 Mar;32(3):893-9. 4. Albert DH, et al. Mol Cancer Ther. 2006 Apr;5(4):995-1006.

Cat. No. Product Name CAS No. Information
GY10559

JTE-952

1255303-54-8

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).

GY04449

Ki20227

623142-96-1

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.

GY01129

BLZ945

953769-46-5

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.

GY01018

Pexidartinib

1029044-16-3

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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