PQR530 是一具有口服活性，种ATP竞争性的，可透过血脑屏障的PI3K/mTORC1/2双重抑制剂，对于 PI3Kα 和 mTOR (分别为 0.84 和 0.33 nM) 的Kd为亚摩尔。它具有抗肿瘤作用。

PQR530 is a highly potent dual pan-PI3K/mTORC1/2 inhibitor. PQR530 inhibited protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation with IC50 values of 0.07 μM. It also showing antitumor activity.

PQR-530 inhibits all PI3K isoforms and mTOR complexes C1/2 potently and selectively. PQR-530 inhibits protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation (IC50: 0.07 μM in A2058 melanoma cells). PQR-530 displays inhibitory activity against the growth of 44 cancer cell lines (mean GI50: 426 nM)[1].

1927857-61-1

C18H23F2N7O2

407.42

PQR-530

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years