Ki20227

製品コードS7688 バッチS768801

化学情報

	Synonyms		Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₄H₂₄N₄O₅S
	分子量	480.54	CAS No.	623142-96-1
Solubility (25°C)*	体外	DMSO	96 mg/mL (199.77 mM)
		Ethanol	3 mg/mL (6.24 mM)
		Water	˂1 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明	Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively.
in vitro	Ki20227, a novel quinoline-urea derivative, is a c-Fms tyrosine kinase inhibitor. The IC50s of Ki20227 to inhibit c-Fms, vascular endothelial growth factor receptor-2 (KDR), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor B are found to be 2, 12, 451, and 217 nmol/L, respectively. Ki20227 is also found to inhibit the M-CSFdependent growth of M-NFS-60 cells but not the M-CSFindependent growth of A375 human melanoma cells in vitro. Furthermore, in an osteoclast-like cell formation assay using mouse bone marrow cells, Ki20227 inhibits the development of tartrate-resistant acid phosphatase-positive osteoclast-like cells in a dose-dependent manner.^[1]
in vivo	In in vivo studies, oral administration of Ki20227 suppresses osteoclast-like cell accumulation and bone resorption induced by metastatic tumor cells in nude rats following intracardiac injection of A375 cells. Moreover, Ki20227 decreases the number of tartrate-resistant acid phosphatase–positive osteoclast-like cells on bone surfaces in ovariectomized (ovx) rats. These findings suggest that Ki20227 inhibits osteolytic bone destruction through the suppression of M-CSF-induced osteoclast accumulation in vivo.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	RAW264.7, M-NFS-60, A375, HUVEC cells
	濃度	0.1 nM - 3000 nM
	反応時間	72 h, 1h
	実験の流れ	M-NFS-60, HUVEC, and A375 cells are seeded on a 96-well culture plate and cultured for 24 hours. Then, culture mediums are changed and incubated for a further 72 hours in the presence or absence of Ki20227 (0.1–3,000 nmol/L). RAW264.7 cells are serum starved for 12 hours in DMEM containing 0.1% FCS. Serial dilutions of Ki20227 are then added to the cells, and they are incubated for 1 hour. RAW264.7 cells are stimulated with 50 ng/mL of recombinant mouse M-CSF for 4 minutes. c-Fms protein in the RAW264.7 cell lysate is prepared with ice-cold lysis buffer.
動物実験	動物モデル	Athymic rats (F344/NJcl-rnu), Sprague-Dawley rats
	投薬量	20 mg/kg
	投与方法	Oral gavage

参考

[1] Hiroaki Ohno, et al. Mol Cancer Ther. 2006 Nov;5(11):2634-43.

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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