Ki20227

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服活性的 c-Fms 抑制剂，IC50 为 2 nM。

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.

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 hourResult:Suppressed M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner.

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.

Ki 20227 | Ki-20227

Tyrosine Kinase

CSF1R

CSF-1R,VEGFR2

Inflammation/Immunology

——

623142-96-1

480.5362

C24H24N4O5S

>98% (HPLC)

DMSO: 7.2 mg/mL

O=C(NC(C1=NC=CS1)C)NC2=CC=C(OC3=CC=NC4=CC(OC)=C(OC)C=C34)C=C2OC

Urea, N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl]-N'-[1-(2-thiazolyl)ethyl]-

(-20℃)

With Ice Pack

≥ 2 years