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PFI-1

CAT: 0013-GTR19163303-02Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163303-02Size:500 mg
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Description
PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM in a cell-free assay. (In Vitro) :PFI-1 has antiproliferative effects on leukemic cell lines and efficiently abrogates their clonogenic growth. Exposure of sensitive cell lines with PFI-1 results in G1 cell-cycle arrest, downregulation of MYC expression, as well as induction of apoptosis and induces differentiation of primary leukemic blasts. Cells exposed to PFI-1 show significant downregulation of Aurora B kinase, thus attenuating phosphorylation of the Aurora substrate H3S10, providing an alternative strategy for the specific inhibition of this well-established oncology target. 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/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.
CAS Number
1403764-72-6
Product Name Alternative
PF-6405761
Purity
>98% (HPLC)
Solubility
DMSO: 69 mg/mL (198.62 mM)
Smiles
O=S (C1=CC=CC=C1OC) (NC2=CC3=C (NC (N (C) C3) =O) C=C2) =O
Molecular Formula
C16H17N3O4S
Molecular Weight
347.39
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2-methoxy-N- (3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl) benzenesulfonamide

Chemical Information

Pfi-1

2-methoxy-N-(3-methyl-2-oxo-1,4-dihydroquinazolin-6-yl)benzenesulfonamide is a member of quinazolines.

CAS Number1403764-72-6
PubChem CID71271629
IUPAC Name2-methoxy-N-(3-methyl-2-oxo-1,4-dihydroquinazolin-6-yl)benzenesulfonamide
Molecular FormulaC16H17N3O4S
Molecular Weight347.4
XLogP1.2
Topological Polar Surface Area96.1
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count5
Rotatable Bond Count4
Heavy Atom Count24
Formal Charge0
Complexity562
SMILES
CN1CC2=C(C=CC(=C2)NS(=O)(=O)C3=CC=CC=C3OC)NC1=O
InChI
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
Chemical Structure
2D Structure
2D structure of Pfi-1
CAS: 1403764-72-6
CID: 71271629
Formula: C16H17N3O4S
MW: 347.4
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight347.4
XLogP31.2
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count5
Rotatable Bond Count4
Exact Mass347.09397721
Monoisotopic Mass347.09397721
Topological Polar Surface Area96.1 Ų
Heavy Atom Count24
Formal Charge0
Complexity562
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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