BV-6

製品コードS7597 バッチS759702

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₇₀H₉₆N₁₀O₈.xCF₃COOH
	分子量	1205.57	CAS No.	1001600-56-1(freebase)
Solubility (25°C)*	体外	DMSO	100 mg/mL (82.94 mM)
		Water	100 mg/mL (82.94 mM)
		Ethanol	100 mg/mL warmed with 50ºC water bath (82.94 mM)
* <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	BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.
in vitro	BV6 inhibits the cell viability of HCC193 NSCLC cells with IC50 of 7.2 μM, induces apoptosis in both HCC193 and H460 cell lines, and also significantly enhances the radiosensitivity of these cell lines through activation of cleaved caspase-8 and cleaved caspase-9, respectively. ^[1] In immature dendritic cells, BV-6 treatment results in moderate activation of the classical NF-kB pathway. ^[2] Furthermore, BV-6 increases CIK cell-mediated lysis of hematological (H9, THP-1, and Tanoue) and solid malignancies (RH1, RH30, and TE671). BV-6 also enhances apoptosis of peripheral blood mononuclear cells and most notably has an inhibitory effect on immune cells limiting their cytotoxic potential. ^[3]
in vivo	BV6 is an IAP antagonist.

製品説明

BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.

in vitro

BV6 inhibits the cell viability of HCC193 NSCLC cells with IC50 of 7.2 μM, induces apoptosis in both HCC193 and H460 cell lines, and also significantly enhances the radiosensitivity of these cell lines through activation of cleaved caspase-8 and cleaved caspase-9, respectively. ^[1]

In immature dendritic cells, BV-6 treatment results in moderate activation of the classical NF-kB pathway. ^[2]

Furthermore, BV-6 increases CIK cell-mediated lysis of hematological (H9, THP-1, and Tanoue) and solid malignancies (RH1, RH30, and TE671). BV-6 also enhances apoptosis of peripheral blood mononuclear cells and most notably has an inhibitory effect on immune cells limiting their cytotoxic potential. ^[3]

in vivo

BV6 is an IAP antagonist.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HCC193 and H460 cells
	濃度	~30 μM
	反応時間	~48 hours
	実験の流れ	Cell viability is measured using the CellTiter 96® Aqueous Non-Radioactive Cell Proliferation Assay kit. 5000 cells/well are seeded into 96-well plates in triplicate. Following adhesion of cells to the wells, increasing concentrations of BV6 are added into different wells. Control groups are exposed to the same concentration of DMSO. The final concentrations of 333 μg/mL MTS and 25 μM PMS are added to each well 24 hours later. After two hours incubation at 37 °C in humidified 5% CO₂, plates are read at the absorbance of 490-nm on a microplate reader. Relative cell viability of an individual sample is calculated by normalizing their absorbance to that of the corresponding control. IC50 values are calculated using Prism 5.01. For the TNFα neutralizing antibody assay, cells are exposed to 1 and 5 μM BV6 with or without 10 μg/mL infliximab and the assay is performed 24 hours later. Plates are read at the absorbance of 490-nm on a microplate reader
動物実験	動物モデル	Female BALB/c mice
	投薬量	10 mg/kg
	投与方法	i.p.

参考

[4] Uegaki T, et al. Hum Reprod. 2015 Jan;30(1):149-58.

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カスタマーフィードバック

: , , FASEB J, 2017, 31(11):4707-4719

: Data from [Data independently produced by , , Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-1548]

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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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