Onalespib（AT13387,ATI13387X）

Biological Activity

AT13387 is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. in vitro: AT13387 is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor AT13387 selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins. AT13387 is a selective potent heat shock protein 90 (Hsp90) inhibitor with IC50 of 18 nM in A375 cells. The Kd for AT13387 binding is 0.7 nM. in vivo: AT13387 could be tolerated at doses of up to 70 mg/kg twice weekly or 90 mg/kg once weekly. Body weight loss in mice does not exceed 20% before recovering in all cases except one, and loss is highest following the second dose. Tumor growth inhibition is similar in NCI-H1975 for both dosing regimens. The maintenance of antitumor effects with such a prolonged off-treatment period is consistent with the extended pharmacodynamic action of AT13387 observed for mutant EGFR and other biomarkers in vitro and in vivo and the extended retention of AT13387 in tumors. For the detailed information of Onalespib（AT13387,ATI13387X）, the solubility of Onalespib（AT13387,ATI13387X） in water, the solubility of Onalespib（AT13387,ATI13387X） in DMSO, the solubility of Onalespib（AT13387,ATI13387X） in PBS buffer, the animal experiment (test) of Onalespib（AT13387,ATI13387X）, the cell expriment (test) of Onalespib（AT13387,ATI13387X）, the in vivo, in vitro and clinical trial test of Onalespib（AT13387,ATI13387X）, the EC50, IC50,and affinity,of Onalespib（AT13387,ATI13387X）, For the detailed information of Onalespib（AT13387,ATI13387X）, the solubility of Onalespib（AT13387,ATI13387X） in water, the solubility of Onalespib（AT13387,ATI13387X） in DMSO, the solubility of Onalespib（AT13387,ATI13387X） in PBS buffer, the animal experiment (test) of Onalespib（AT13387,ATI13387X）, the cell expriment (test) of Onalespib（AT13387,ATI13387X）, the in vivo, in vitro and clinical trial test of Onalespib（AT13387,ATI13387X）, the EC50, IC50,and affinity,of Onalespib（AT13387,ATI13387X）, Please contact DC Chemicals.

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.