Izorlisib

The deregulation of phosphatidylinositol 3-kinase (PI3K)/Akt pathway is commonly seen in various human cancers. CH5132799 is a PI3K inhibitor that inhibits PI3Kα, β, δ, γ with IC50 values of 14 nM, 0.12 mM, 0.5 mM and 36 nM, respectively. In breast cancer KPL-4 cells harboring PIK3CA mutation, treatment of 0.001 – 10 mM CH5132799 for 2h suppressed the phosphorylation of Akt and its downstream factors, S6K, S6 and 4E-BP1. When KPL-4 cells were treated with 1 mM CH5132799 for 48h, the G₁ arrest and Caspase 3/7 activity were induced. CH5132799 also demonstrated anti-proliferative effect in 60 breast, ovarian, prostate, and endometrial cancer cell lines with 75% of lines having an IC50 value less than 1mM and 38% of lines having an IC50 under 0.3 mM. In the xenograft model of KPL-4 cells harboring the PIK3CA H1047R mutation, daily oral administration of CH5132799 (0.39 – 25 mg/kg/day) showed anti-tumor effect since day 21 post tumor implantation. The inhibition of the PI3K pathway and Akt phosphorylation were also observed in this xenografts model treated by CH5132799. Oral administration of CH5132799 (12.5 mg/kg/day, 12 consecutive days) in mice bearing trastuzumab-insensitive KPL-4 tumors induced remarkable reduction in the tumor volume, and eventually the disappearance of the tumors³.

溶解方案(细胞实验)

DMSO 中的溶解度 : 4.55 mg/mL (12.06 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 0.46 mg/mL (1.22 mM); 澄清溶液 此方案可获得 ≥ 0.46 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 4.6 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"