- 体外研究
在含PtdIns(3,4,5)P
3
465E/K465E
2+
2+
- 靶点
IC50: 10 nM(PDK1)
- 体内研究
Braf
V600E
::Pten
−/−
mice subjected to systemic administration of 4-HT. Twice weekly administration of PDK1 results in marked inhibition of pigmented lesions and concomitant melanomagenesis, as well as significant inhibition of lung metastases, seen by H&E staining-based quantification (~80%), and lymph node metastases as by S100 immunostaining, similar to the phenotype seen upon genetic ablation of
Pdk1
.
