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SML2674

Sigma-Aldrich

Ki20227

≥98% (HPLC)

Sinônimo(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

Fórmula empírica (Notação de Hill):
C24H24N4O5S
Número CAS:
623142-96-1
Peso molecular:
480.54
Número MDL:
MFCD12024693
Código UNSPSC:
12352200
NACRES:
NA.77

Ensaio

≥98% (HPLC)

forma

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear

temperatura de armazenamento

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)

chave InChI

SHPFDGWALWEPGS-UHFFFAOYSA-N

Ações bioquímicas/fisiológicas

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.

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 1

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Certificados de análise (COA)

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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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