Decrease in phosphorylated ERK indicates the therapeutic efficacy of a clinical PI3K α-selective inhibitor CYH33 in breast cancer

PI3Ks are frequently hyper-activated in breast cancer and targeting PI3K α has exhibited promising but variable response in preclinical and clinical settings. CYH33 is a novel PI3Kα-selective inhibitor in phase I clinical trial. We investigated the efficacy of CYH33 against breast cancer and explored potential predictive biomarkers. CYH33 potently restrained tumor grow th in mice bearing human breast cancer cell xenografts and in R26-Pik3caH1047R;MMTV-Cre transgenic mice. CYH33 significantly inhibited proliferation of a panel of human breast cancer cells, while diversity in sensitivity has been observed.
Source: Cancer Letters - Category: Cancer & Oncology Authors: Tags: Original Articles Source Type: research