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SNG1153 is a synthetic ER-α36 modulator, showed promising activities in many in vitro and in vivo models. In-vivo efficacies of SNG1153 were evaluated in Bcap-37 xenograft model, Ishikawa xenograft model and SPC-A-1 xenograft model. Results: SNG1153 showed significant inhibition at low micromolar concentrations in ER-α36 overexpressed cell lines including the one resistant to tamoxifen. SNG1153 exhibited a linear PK profile with a bioavailability of more than 55% in the rat PK study. In the in-vivo efficacy studies, 3 doses were investigated and SNG1153 showed dose-dependent inhibition. The tumor growth inhibition at high dose was 57% in the breast cancer Bcap-37 xenograft model, 65% in the endometrial cancer Ishikawa xenograft model and 52% in lung adenocarcinoma SPC-A-1 xenograft model. No signs of toxicity were observed in these model. For the detailed information of SNG-1153, the solubility of SNG-1153 in water, the solubility of SNG-1153 in DMSO, the solubility of SNG-1153 in PBS buffer, the animal experiment (test) of SNG-1153, the cell expriment (test) of SNG-1153, the in vivo, in vitro and clinical trial test of SNG-1153, the EC50, IC50,and affinity,of SNG-1153, For the detailed information of SNG-1153, the solubility of SNG-1153 in water, the solubility of SNG-1153 in DMSO, the solubility of SNG-1153 in PBS buffer, the animal experiment (test) of SNG-1153, the cell expriment (test) of SNG-1153, the in vivo, in vitro and clinical trial test of SNG-1153, the EC50, IC50,and affinity,of SNG-1153, Please contact DC Chemicals. |