Name | BV6 |
Synonyms | BV6 BV-6 CS-1501 CS-2877 BV-6 BV 6 4,4'-(1,6-Hexanediyl)bis[N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-L-prolyl-beta-phenyl-L-phenylalaninamide |
CAS | 1001600-56-1 |
Molecular Formula | C70H96N10O8 |
Molar Mass | 1205.57 |
Density | 1.177±0.06 g/cm3(Predicted) |
Boling Point | 1376.7±65.0 °C(Predicted) |
Solubility | DMSO: ≥ 58 mg/mL |
pKa | 12.89±0.20(Predicted) |
Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
In vitro study | BV6 inhibited the cell activity of HCC193 NSCLC cells with IC50 of 7.2 μm and caused apoptosis in HCC193 and H460 cell lines, the radiosensitivity of these cell lines was significantly increased by activating lysed caspase-8 and caspase-9, respectively. In immature dendritic cells, BV-6 treatment resulted in modest activation of the classical NF-kB pathway. In addition, BV-6 increased CIK cell-mediated regression of hematologic disorders (H9,THP-1, and Tanoue) and solid tumors (RH1,RH30, and TE671). BV-6 also enhances apoptosis of peripheral blood mononuclear cells and has a significant inhibitory effect on immune cells limiting their cytotoxic potential. |
In vivo study | Murine cIAP-1, cIAP-2 and XIAP expressions are clearly observed in the cytoplasm of both epithelial and stromal cells of implants, whereas Survivin is mainly expressed in the nuclei BV6 treatment for 4 weeks attenuated the intensity of IAPs expression. The size of lesions range from ~2 to 7 mm in diameter. The monolayer epithelial cell lining of the cyst is shown. After immunohistochemical staining, cytokeratin and vimentin are positively stained, whereas calretinin is negative. After BV6 treatment for 4 weeks, the total number of lesions (4.6 versus 2.8/mouse), the average weight (78.1 versus 32.0 mg/mouse) and the surface area (44.5 versus 24.6 mm 2 /mouse) of lesions are significantly less than in the controls. In the endometrial gland epithelia or stroma, the percentage of Ki67-positive cells decreases after BV6 treatment. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 0.829 ml | 4.147 ml | 8.295 ml |
5 mM | 0.166 ml | 0.829 ml | 1.659 ml |
10 mM | 0.083 ml | 0.415 ml | 0.829 ml |
5 mM | 0.017 ml | 0.083 ml | 0.166 ml |
biological activity | BV-6 is a SMAC-mimicking dual inhibitor of cIAP and XIAP. |
Target | IAP |