LY2940680 1258861-20-9

LY2940680  1258861-20-9

LY-2940680
分子式：C26H24F4N6O   分子量：512.5
 
产品描述
LY2940680 与 Smoothened(Smo)受体结合，有效抑制Hedgehog(Hh)信号通路。
靶点
Smo
         
IC50
           
体外研究
LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib.
体内研究
LY2940680 has excellent pharmacokinetic properties in rodent and non-rodent species. LY2940680 administrated orally treats Ptch+/- p53-/- transgenic mice which spontaneously develop medulloblastoma, produces remarkable efficacy and significantly improves their survival. LY2940680 reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and LY2940680 induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. LY2940680 inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity.
溶解性
DMSO 0.66 mg/mL，水 <1 mg/mL，乙醇 2 mg/mL
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO