PFI-1
PFI-1 Basic information
- Product Name:
- PFI-1
- Synonyms:
-
- PFI-1
- PFI-1 (PF-6405761)
- PFI-1 (PF-06405761)
- PFI 1;PFI1
- CS-709
- PF-06405761
- Benzenesulfonamide, 2-methoxy-N-(1,2,3,4-tetrahydro-3-methyl-2-oxo-6-quinazolinyl)-
- 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide PFI-1 (PF-6405761)
- CAS:
- 1403764-72-6
- MF:
- C16H17N3O4S
- MW:
- 347.39
- Product Categories:
-
- Inhibitors
- Inhibitor
- Mol File:
- 1403764-72-6.mol
PFI-1 Chemical Properties
- storage temp.
- Sealed in dry,2-8°C
- solubility
- DMSO: ≥10mg/mL
- form
- powder
- color
- white to beige
PFI-1 Usage And Synthesis
Description
PFI 1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. PFI-1 is a selective BET bromodomain inhibitor with activity at BRD2 (IC50 = 98 nM) and BRD4 (IC50 = 220 nM). PFI 1 induces apoptosis and G1 cell cycle arrest in BET inhibitor-sensitive cell lines (MV4;11). PFI 1 also downregulates Aurora B expression in MV4;11 cells.
Uses
PFI-1 is used as a selective protein interaction inhibitor targetting BET bromodomains, used as regulators required for efficient expression of several growth promoting and anti-apoptotic genes.
Definition
ChEBI: 2-methoxy-N-(3-methyl-2-oxo-1,4-dihydroquinazolin-6-yl)benzenesulfonamide is a member of quinazolines.
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/kg 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[2].
storage
Store at RT
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