An inhibitor of IRAK4 (IC50 = 0.2 nM in a cell-free assay); inhibits 100% of IRAK4 activity and is selective for IRAK4 over 273 kinases in a panel at 200 nM

PF-06650833 – 10 mg

Brand:
Cayman
CAS:
1817626-54-2
Storage:
-20
UN-No:
Non-Hazardous - /

PF-06650833 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4; IC50 = 0.2 nM in a cell-free assay).{46434} It inhibits 100% of IRAK4 activity and is selective for IRAK4 over 273 kinases in a panel at 200 nM, but does inhibit IRAK1, MNK2, LRRK2, CLK4, and CLKɣ1 activity by greater than 70%. PF-06650833 reduces levels of TNF-α and IL-6 in R848-stimulated isolated human whole blood and peripheral blood mononuclear cells (PBMCs), respectively (IC50 = ~2 nM for both). It decreases LPS-induced increases in rat serum levels of TNF-α when administered at doses of 1, 3, and 30 mg/kg.  

 

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SKU: 28397 - 10 mg Category:

Description

An inhibitor of IRAK4 (IC50 = 0.2 nM in a cell-free assay); inhibits 100% of IRAK4 activity and is selective for IRAK4 over 273 kinases in a panel at 200 nM, but does inhibit IRAK1, MNK2, LRRK2, CLK4, and CLKɣ1 activity by greater than 70%; reduces levels of TNF-α and IL-6 in R848-stimulated isolated human whole blood and peripheral blood mononuclear cells (PBMCs), respectively (IC50 = ~2 nM for both); decreases LPS-induced increases in rat serum levels of TNF-α when administered at 1, 3, and 30 mg/kg.

Formal name: 1-[[(2S,3S,4S)-3-ethyl-4-fluoro-5-oxo-2-pyrrolidinyl]methoxy]-7-methoxy-6-isoquinolinecarboxamide

Synonyms: 

Molecular weight: 361.4

CAS: 1817626-54-2

Purity: ≥98%

Formulation: A solid

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