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Merck
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SML2674

Sigma-Aldrich

Ki20227

≥98% (HPLC)

Synonyme(s) :

Ki 20227, N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl]-N′-[1-(2-thiazolyl)ethyl]urea, N-{4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl}-N′-[1-(1,3-thiazol-2-yl)ethyl]urea

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About This Item

Formule empirique (notation de Hill):
C24H24N4O5S
Numéro CAS:
623142-96-1
Poids moléculaire :
480.54
Numéro MDL:
MFCD12024693
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

InChI

1S/C24H24N4O5S/c1-14(23-26-9-10-34-23)27-24(29)28-17-6-5-15(11-20(17)30-2)33-19-7-8-25-18-13-22(32-4)21(31-3)12-16(18)19/h5-14H,1-4H3,(H2,27,28,29)

Clé InChI

SHPFDGWALWEPGS-UHFFFAOYSA-N

Actions biochimiques/physiologiques

Ki20227 is an orally active, potent and selective M-CSF receptor c-Fms (CSF-1R) tyrosine kinase inhibitor (IC50 = 2 nM vs. 12 nM/KDR, 451 nM/c-Kit, 217 nM/PDGFβ; >1 μM/BTK, EGFR, FGFR2, FLT3, Fyn, Met, c-Src, PKA, PKCα) that inhibits M-CSF-dependent (50 ng/mL) c-Fms phosphorylation (by >90% at 10 nM; RAW264.7) and cell growth (IC50 = 14 nM; M-NFS-60). Ki20227 prevents osteolysis in a rat model of bone metastasis (50 mg/kg/day p.o.) by inhibiting A375 tumor-induced osteoclast formation and decreases the number of osteoclast-like cells on bone surfaces in ovariectomized rats (20 mg/kg/day p.o.) in vivo.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 1

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Kelda Chia et al.
eLife, 7 (2018-02-22)
It is now clear that microglia and macrophages are present in brain tumors, but whether or how they affect initiation and development of tumors is not known. Exploiting the advantages of the zebrafish (Danio rerio) model, we showed that macrophages
Igor Theurl et al.
Nature medicine, 22(8), 945-951 (2016-07-19)
Iron is an essential component of the erythrocyte protein hemoglobin and is crucial to oxygen transport in vertebrates. In the steady state, erythrocyte production is in equilibrium with erythrocyte removal. In various pathophysiological conditions, however, erythrocyte life span is compromised
Hiroaki Ohno et al.
Molecular cancer therapeutics, 5(11), 2634-2643 (2006-11-24)
In bone metastatic lesions, osteoclasts play a key role in the development of osteolysis. Previous studies have shown that macrophage colony-stimulating factor (M-CSF) is important for the differentiation of osteoclasts. In this study, we investigated whether an inhibitor of M-CSF
Hiroaki Ohno et al.
European journal of immunology, 38(1), 283-291 (2007-12-19)
Macrophage colony-stimulating factor (M-CSF) is important in the development of macrophages and osteoclasts. Previous studies have also shown that CD11b(+) myeloblasts and osteoclasts play key roles during inflammation and bone destruction in arthritic lesions. In this study, we investigated whether
Yasunori Uemura et al.
Journal of neuroimmunology, 195(1-2), 73-80 (2008-04-02)
Experimental autoimmune encephalomyelitis (EAE), an animal model of multiple sclerosis (MS), can be induced by the immunization of mice with myelin antigens in the form of myelin oligodendrocyte glycoprotein (MOG). Macrophage colony-stimulating factor (M-CSF) is required for the development of
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