中文名：PFI-1 (PF-6405761)
英文名：PFI-1 (PF-6405761)
英文別名：Benzenesulfonamide, 2-methoxy-N-(1,2,3,4-tetrahydro-3-methyl-2-oxo-6-quinazolinyl)-
純度：10mM in DMSO
貨號：P408161
包裝：1ml
Cas號：1403764-72-6
存儲溫度：-80℃儲存
產(chǎn)品介紹：
Information
PFI-1 (PF-6405761) PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay.
In?vitro
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).
In?vivo
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.
Cell?Data
cell?lines：
Concentrations：1 mM
Incubation?Time：5 days
Powder?Purity:≥96%
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關(guān)鍵字： Benzenesulfonamide, 2-methoxy-N-(1,2,3,4-tetrahydro-3-methyl-2-oxo-6-quinazolinyl)-
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