Ki20227

SKU: orb1224427

Description

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.

Key Properties

• CAS Number: 623142-96-1
• MW: 480.5362
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₄N₄O₅S
• SMILES: O=C(NC(C1=NC=CS1)C)NC2=CC=C(OC3=CC=NC4=CC(OC)=C(OC)C=C34)C=C2OC
• Target: CSF1R
• Solubility: DMSO: 7.2 mg/mL

Bioactivity

• In Vivo:
  Ki20227 (orally; 10-50 mg/kg/d for 20 days) of 50 mg/kg/d of Ki20227 for 20 days markedly decreases the osteolytic lesion areas. ki20227 during global ischemia led to a significant deficit in microglial density in the CNS in mice, and CSF1R-inhibition led to a significant reduction in the neuronal density of mice. Animal model: 4-week-old male F344/NJcl-rnu rats. Dosage: 10, 20, and 50 mg/kg. Administration: Orally; once per day for 20 days. Result: Oral administration of 50 mg/kg/d markedly decreased the osteolytic lesion areas.
• In Vitro:
  Ki20227 (0.1-1000 nM; 72 hours) with 100 and 1, 000 nM almost suppresses M-NFS-60 cell growth and HUVEC cell growth, respectively. Ki20227 (0.1-1000 nM; 1 hour) suppresses M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner. Cell Viability Assay Cell line: M-NFS-60 cells, HUVEC cells, human A375 melanoma cells. Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM Incubation time: 72 hours. Result: 100 and 1, 000 nM almost suppressed M-NFS-60 cell growth and HUVEC cell growth, respectively. Cell Viability Assay Cell line: RAW264.7 cell lysate Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM Incubation time: 1 hour. Result: Suppressed M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ki 20227 | Ki-20227

Quick Database Links

Gene Symbol

CSF1R