Ki20227

SKU: orb1302959

Description

Ki-20227 is a potent and selective small molecule inhibitor of the c-Fms/CSF1R tyrosine kinase with an IC50 of 2 nM. It also exhibits activity against VEGFR2 and c-Kit/PDGFRβ. This inhibitor is a valuable research tool for studying tumor-associated macrophages, angiogenesis, and related oncogenic pathways in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 623142-96-1
• MW: 480.54
• Purity: 99.88% (May vary between batches)
• Formula: C₂₄H₂₄N₄O₅S
• SMILES: COc1cc(Oc2ccnc3cc(OC)c(OC)cc23)ccc1NC(=O)NC(C)c1nccs1
• Target: CSF-1R,VEGFR,c-Fms,c-Kit,PDGFR
• Solubility: DMSO:55 mg/mL (114.45 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.16 mM)

Bioactivity

• Target IC50:
  VEGFR2:12 nM|CSF1R:2 nM
• In Vivo:
  Ki20227 reduces the number of tartrate-resistant acid phosphatase-positive osteoclast-like cells on bone surfaces in ovariectomized (ovx) rats. Furthermore, in the Ki20227-treated mice, the number of CD11b(+), Gr-1(+), and Ly-6 g(+) cells in the spleen were decreased and the CII-induced cytokine production in splenocytes isolated from the Ki20227-treated arthritic mice was also reduced. In EAE animal model, Ki20227 inhibits the turn-over/expansion of myeloid cells provoked by the immunization and subsequent MOG-specific T cell responses.
• In Vitro:
  Ki20227 hasn't inhibition for other kinases tested, such as EGFR, Fms-like tyrosine kinase-3, or c-Src (c-src proto-oncogene product). Ki20227 also inhibits the M-CSF-dependent growth of M-NFS-60 cells but not the M-CSF-independent growth of A375 human melanoma cells in vitro. Ki20227 has an inhibition against M-CSF-dependent reactions, such as lipopolysaccharide-induced TNF-α production, which was enhanced by M-CSF in vitro.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CSF-1 receptor, CSF1R, CSF-1R, CD117, c-Fms, cFms, colony stimulating factor 1 receptor, cKit, c-Kit, Inhibitor, Platelet-derived growth factor receptor, Ki 20227, Ki-20227, Ki20227, inhibit, SCFR, PDGFR, Vascular endothelial growth factor receptor, VEGFR, VEGFR2

Compound Identifiers

PubChem CID

9869779