PQR620 是一种可透过血脑屏障的，具有口服活性的mTORC1/2选择性抑制剂。

PQR620 is a novel potent and selective, brain penetrant inhibitor of mTORC1/2.

PQR620 is a potent and selective mTOR inhibitor, which induces >1000-fold selectivity towards mTOR over PI3Kα in enzymatic binding assays.?In A2058 melanoma cells PQR620 demonstrates inhibition of protein kinase B (pSer473) and ribosomal protein S6 (pSer235/236) phosphorylation with IC50 values of 0.2 μM and 0.1 μM, respectively.?PQR620 shows excellent selectivity over a wide panel of kinases, as well as excellent selectivity versus unrelated receptor enzymes and ion channels.?PQR620 demonstrates its potency to prevent cancer cell growth in an NTRC 44 cancer cell line panel, resulting in a 10log(IC50) of 2.86 (nM).

The physico-chemical properties of PQR620 result in good oral bioavailability and excellent brain penetration.

1927857-56-4

C21H25F2N7O2

445.475

DMSO:6.4 mg/mL (14.37 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years