PF-06650833

• CAT Number: I002359
• CAS Number: 1817626-54-2
• Molecular Formula: C₁₈H₂₀FN₃O₄
• Molecular Weight: 361.37
• Purity: ≥95%
• Synonyms: PF-06650833; 1-[[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxo-2-pyrrolidinyl]methoxy]-7-methoxy-6-isoquinolinecarboxamide
• Target: IRAK4
• Solubility: DMSO: ≥ 33 mg/mL
• Storage: Store at -20°C
• InChI: InChI=1S/C18H20FN3O4/c1-3-10-13(22-17(24)15(10)19)8-26-18-11-7-14(25-2)12(16(20)23)6-9(11)4-5-21-18/h4-7,10,13,15H,3,8H2,1-2H3,(H2,20,23)(H,22,24)/t10-,13+,15-/m0/s1
• SMILES: O=C(C1=CC2=C(C(OC[[email protected]]([[email protected]](CC)[[email protected]@H]3F)NC3=O)=NC=C2)C=C1OC)N

PF06650833(CAT: I002359) is an inhibitor of Interleukin-1 receptor-associated kinase 4 (IRAK4). It is a small molecule drug that specifically targets IRAK4, which plays a crucial role in the signaling pathways of the innate immune system. By inhibiting IRAK4, PF06650833 can modulate the inflammatory response and immune system activity. This makes it a potential therapeutic option for the treatment of various diseases characterized by dysregulated immune responses, such as rheumatoid arthritis, lupus, and lymphomas.

Reference

1. Expert Opin Ther Pat. 2016 Aug;26(8):917-32. doi: 10.1080/13543776.2016.1202926.
Epub 2016 Jun 29.

Inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4): a patent review
(2012-2015).

Seganish WM(1).

Author information:
(1)a Discovery Chemistry , Merck Sharp and Dohme Corp ., Kenilworth , NJ , USA.

INTRODUCTION: IRAK4 is located proximal to TLR/IL-1 receptors, and in preclinical
studies, inhibits downstream signaling from these receptors. The development of
novel small molecule inhibitors of this kinase has the potential to lead to new
therapeutics to treat diseases such as rheumatoid arthritis, lupus, and
lymphomas.
AREAS COVERED: The aim of this review is to summarize the recent patent
literature (2012-2015) surrounding small molecule inhibitors of IRAK4. Specific
examples of the chemical matter from each patent will be discussed, including any
data that are presented for the examples highlighted.
EXPERT OPINION: There are currently many examples of highly potent and kinase
selective IRAK4 inhibitors and some have been tested in various in vivo disease
models, demonstrating robust pre-clinical efficacy. Several compounds appear to
have the /’drug-like/’ properties to advance to the clinic, with Pfizer having
already initiated several phase I studies.