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VER-155008 is a novel, small molecule inhibitor of Hsc70/Hsp70 with GI50 of 5.3-14.4 uM in human breast and colon cancer cell lines.in vitro: VER-155008 inhibited the proliferation of human breast and colon cancer cell lines with GI(50)s in the range 5.3-14.4 microM, and induced Hsp90 client protein degradation in both HCT116 and BT474 cells. As a single agent, VER-155008 induced caspase-3/7 dependent apoptosis in BT474 cells and non-caspase dependent cell death in HCT116 cells. VER-155008 potentiated the apoptotic potential of a small molecule Hsp90 inhibitor in HCT116 but not HT29 or MDA-MB-468 cells. VER-155008 (HCT116 GI50 = 5 μM), has similar potencies in both Grp78 and Hsp70. Inhibition of Hsp70/Hsc70 activity with VER 155008 attenuated the protection afforded by N-acetyl cysteine in a dose-responsive manner.
in vivo: VER-155008 demonstrated rapid metabolism and clearance, along with tumor levels below the predicted pharmacologically active level. For the detailed information of VER155008, the solubility of VER155008 in water, the solubility of VER155008 in DMSO, the solubility of VER155008 in PBS buffer, the animal experiment (test) of VER155008, the cell expriment (test) of VER155008, the in vivo, in vitro and clinical trial test of VER155008, the EC50, IC50,and affinity,of VER155008, For the detailed information of VER155008, the solubility of VER155008 in water, the solubility of VER155008 in DMSO, the solubility of VER155008 in PBS buffer, the animal experiment (test) of VER155008, the cell expriment (test) of VER155008, the in vivo, in vitro and clinical trial test of VER155008, the EC50, IC50,and affinity,of VER155008, Please contact DC Chemicals. |