For research use only.
CAS No. 1817626-54-2
PF-06650833 is a potent, selective inhibitor of IRAK4 with an IC50 of 0.2 nM.
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|Description||PF-06650833 is a potent, selective inhibitor of IRAK4 with an IC50 of 0.2 nM.|
The kinome selectivity profile of PF-06650833 is assessed in a panel of 278 kinases(Invitrogen) at 200 nM inhibitor concentration using the ATP Km for each kinase. Approximately 100% inhibition is observed for IRAK4 while greater than 70% inhibition is observed for the following kinases, in order of potency: IRAK1, MNK2, LRRK2, CLK4, and CK1γ1. Lactam PF-06650833 is subsequently assessed in a whole cell functional VEGF2R assay (PAE-KDR cell line). No activity was observed at concentrations up to and including 30 µM. .
PF-06650833 significantly inhibits LPS-induced TNF in a dose dependent manner. Mean exposures of PF-06650833 in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration of PF-06650833 at 0.3 mg/kg, 1 mg/kg, 3 mg/kg and 30 mg/kg. The fraction unbound in rat plasma of PF-06650833 is 0.3.
|In vitro||DMSO||72 mg/mL (199.24 mM)|
|Ethanol||3 mg/mL (8.3 mM)|
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