| Identification | Back Directory | [Name]
PFI-1 | [CAS]
1403764-72-6 | [Synonyms]
PFI-1
CS-709
PFI 1;PFI1
PF-6405761
PF-06405761
PFI-1 USP/EP/BP
PFI-1 (PF-6405761)
PFI-1 (PF-06405761)
PFI-1;PFI-1;PFI 1;PFI1
2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydro-quinazolin-6-yl)-bezenesulfonamide
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) | [Molecular Formula]
C16H17N3O4S | [MDL Number]
MFCD22580416 | [MOL File]
1403764-72-6.mol | [Molecular Weight]
347.39 |
| Chemical Properties | Back Directory | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO: ≥10mg/mL | [form ]
powder | [color ]
white to beige | [InChI]
1S/C16H17N3O4S/c1-19-10-11-9-12(7-8-13(11)17-16(19)20)18-24(21,22)15-6-4-3-5-14(15)23-2/h3-9,18H,10H2,1-2H3,(H,17,20) | [InChIKey]
TXZPMHLMPKIUGK-UHFFFAOYSA-N | [SMILES]
COc1ccccc1S(=O)(=O)Nc2ccc3NC(=O)N(C)Cc3c2 |
| Hazard Information | Back Directory | [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 -20°C |
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