| Identification | Back Directory | [Name]
PF 184 | [CAS]
1187460-81-6 | [Synonyms]
PF 184
8-[[[5-Chloro-2-[3,4-diMethyl-3,4-bis(hydroxyMethyl)-1-pyrrolidinyl]-4-pyridinyl]carbonyl]aMino]-1-(4-fluorophenyl)-4,5-dihydro-1H-benz[g]indazole-3-carboxaMide
1H-Benz[g]indazole-3-carboxamide, 8-[[[2-[3,4-bis(hydroxymethyl)-3,4-dimethyl-1-pyrrolidinyl]-5-chloro-4-pyridinyl]carbonyl]amino]-1-(4-fluorophenyl)-4,5-dihydro- | [Molecular Formula]
C32H32ClFN6O4 | [MDL Number]
MFCD17166976 | [MOL File]
1187460-81-6.mol | [Molecular Weight]
619.09 |
| Chemical Properties | Back Directory | [Boiling point ]
790.6±60.0 °C(Predicted) | [density ]
1.47±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble to 100 mM in DMSO | [form ]
Powder | [pka]
10.20±0.20(Predicted) |
| Hazard Information | Back Directory | [Uses]
PF 184 is a potent and selective IKK-2 inhibitor (IC50 = 37 nM). Displays selectivity over 85 other kinases. Inhibits IL-1β-induced TNF-α in a steroid-insensitive in vitro model of oxidative stress. | [in vivo]
(Rac)-PF-184 (0.3-2.5 mg; i.t.; once) blocks neutrophil infiltration and BAL cell cytokine production[1]. | Animal Model: | Fasted male Sprague-Dawley rats (350 g) placed into a chamber connected to a large volume nebulizer filled with 20 ml of 1 mg/mL solution of LPS[1] | | Dosage: | 0.3-2.5 mg | | Administration: | Nano suspension and administered intratracheally in a volume of 100 μL, 60 min before aerosolized LPS | | Result: | Resulted in a comparable attenuation of total cell and PMN cell infiltration 4 h after LPS exposure. Dose-dependently inhibited cell infiltration with EC50 values of 1 mg. Dose-dependently suppressed BAL fluid TNF- and PGE2 levels comparable with cell infiltration. Inhibited p65 translocation. Showed long-lasting activity. |
| [IC 50]
IKK-2: 37 nM (IC50) | [storage]
Store at -20°C |
|
|