XRK3F2

製品コードS8756 バッチS875601

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₃H₂₄ClF₂NO₃
	分子量	435.89	CAS No.	2375193-43-2
Solubility (25°C)*	体外	DMSO	87 mg/mL (199.59 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	XRK3F2 is an inhibitor of the p62-ZZ domain that blunts MM-induced Runx2 suppression in vitro, and induces new bone formation and remodeling in the presence of tumor in vivo.
in vitro	XRK3F2 blocks TNFα and MM (Multiple myeloma) activation of downstream signaling from the p62-signaling hub. In addition, XRK3F2 also directly decreases osteoclast formation. It directly inhibits cell growth of primary CD138+ MM cells and human MM cell lines in vitro, without negatively affecting the growth of BMSC^[1]. XRK3F2 has no effect on non-MM bearing bone. XRK3F2 blocks TNFα but not IL-1β stimulated NFκB phosphorylation in MM patient BMSC and inhibits IκBα degradation by interfering with p-IκBα activation in MM cells treated with TNFα. XRK3F2 also significantly inhibits TNFα-enhanced VCAM-1, IL-6, and RANKL expression by BMSCs from MM patients compared to vehicle. XRK3F2 directly activates caspases 3, 7, and 9 in MM cells and decreases NFκB signaling in MM results in the aggregation of caspase 8 and its downstream effector caspases. Thus, high concentrations of XRK3F2 induce apoptosis in MM cells^[2].
in vivo	In vivo, XRK3F2 induces new bone formation and remodeling in the presence of tumor. The t_1/2 of XRK3F2 in mice is 10.3 hours. XRK3F2 induces dramatic, local new bone formation in bones bearing MM in vivo but does not induce new bone formation in bones from the same animals that are not directly inoculated with MM cells. The results demonstrate that XRK3F2 alters the effect of MM on bone^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MC4 cells
	濃度	5 μM
	反応時間	48 h
	実験の流れ	MC4 cells are cultured in with or without 5TGM1 MM cells (in direct contact) for 48 h under proliferation conditions +/– XRK3F2 (5 μM). MM cells are then removed by washing and media is changed to osteogenic differentiation conditions +/– XRK3F2. MC4 cells are collected at the time of MM cell removal (day 0), and after 4 days of differentiation culture in the absence of MM cells (day 4).
動物実験	動物モデル	Specific-pathogen-free, male C57BL/KaLwRij mice (6–12 weeks of age) with implanted tumor
	投薬量	27 mg/kg/day or 40 mg/kg/day
	投与方法	i.p.

参考

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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