PFI-1（PF-6405761）是一种选择性BET (包含溴结构域蛋白)抑制剂，作用于BRD4，无细胞试验中IC50为0.22 μM。

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

PFI 1; PFI1

DMSO Solubility: 69 mg/mL (198.62 mM)

BRD2 ,BRD4

PFI-1 binds to with cyclic AMP response binding protein with KD of 49 μM. PFI-1 has an EC50 of 1.89 μM for the inhibition of IL6 production from human blood mononuclear cells stimulated by LPS. PFI-1 induces dose-dependent reduction of cell viability in T4302 CD133+ cells. PFI-1 inhibits the proliferating of three NET cell lines (Bon-1 derived from a pancreatic NET, and H727 and H720 derived from lung NETs).

PFI-1 administrated (1 mg/kg i.v.) in the rat results in the volume of distribution of 1 L/kg, the plasma clearance of 18/mL·min–1·kg–1 and half-life of 1 hour. PFI-1 oral dosed (2 mg/kg) in the rat results in the oral bioavailability as low as 32%. PFI-1 administrated (2 mg/kg s.c.) in the mouse results in a Cmax of 58 ng/mL with a Tmax of 1 h and a half-life of approximately 2 hours.

[1] Fish PV, et al. J Med Chem, 2012, 55(22), 9831-9837.

[2] Cheng Z, et al. Clin Cancer Res, 2013, 19(7), 1-12.