BV-6 1001600-56-1

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Molecular Weight:

1205.57 BV-6 is a SMAC mimetic, dual cIAP and XIAP Inhibitor.


Biological Activity


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


Protocol(Only for Reference)


Cell Assay: [1]

Cell lines	HCC193 and H460 cells
Concentrations	~30 μM
Incubation Time	~48 hours
Method	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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	1205.57
Formula	C70H96N10O8
CAS No.	1001600-56-1

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	N/A

Solubility (25°C) *	In vitro	DMSO	100 mg/mL (82.94 mM)
		Water	25 mg/mL (20.73 mM)
		Ethanol	100 mg/mL heating (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.

Chemical Name	N,N'-(hexane-1,6-diyl)bis(1-{(2S)-2-cyclohexyl-2-[(N-methyl-L-alanyl)amino]acetyl}-L-prolyl-beta-phenyl-L-phenylalaninamide)

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Product Categories : Apoptosis > IAP Inhibitor