LY2940680  1258861-20-9

LY-2940680
分子式：C26H24F4N6O   分子量：512.5
 
產(chǎn)品描述
LY2940680 與 Smoothened(Smo)受體結(jié)合，有效抑制Hedgehog(Hh)信號(hào)通路。
靶點(diǎn)
Smo
         
IC50
           
體外研究
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.
體內(nèi)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
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO