WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 327020
Description: Poseltinib, also known HM-71224, LY3337641 and PRN1008, is a tyrosine kinase inhibitor. Poseltinib is an experimental Bruton's tyrosine kinase inhibitor for the treatment of rheumatoid arthritis. HM71224 irreversibly bound to and inhibited Btk (IC50 = 1.95 nM). The compound also inhibited the phosphorylation of Btk and its downstream molecules such as PLCγ2, in activated Ramos B lymphoma cells and primary human B cells in a dose-dependent manner. Furthermore, HM71224 effectively inhibited the production of tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-1β by human monocytes, and osteoclast formation by human monocytes. HM71224 inhibits Btk in B cells and monocytes and ameliorates experimental arthritis in a mouse model. HM71224 is a potential novel therapeutic agent for rheumatoid arthritis in humans.
MedKoo Cat#: 327020
Chemical Formula: C26H26N6O3
Exact Mass: 470.2066
Molecular Weight: 470.533
Elemental Analysis: C, 66.37; H, 5.57; N, 17.86; O, 10.20
Synonym: Poseltinib; HM 71224; HM-71224; HM71224; LY 3337641; LY3337641; LY-3337641; PRN1008; PRN-1008; PRN 1008.
IUPAC/Chemical Name: N-(3-((2-((4-(4-methylpiperazin-1-yl)phenyl)amino)furo[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide
InChi Key: LZMJNVRJMFMYQS-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H26N6O3/c1-3-23(33)27-19-5-4-6-21(17-19)35-25-24-22(11-16-34-24)29-26(30-25)28-18-7-9-20(10-8-18)32-14-12-31(2)13-15-32/h3-11,16-17H,1,12-15H2,2H3,(H,27,33)(H,28,29,30)
SMILES Code: C=CC(NC1=CC=CC(OC2=C(OC=C3)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O
1: Park JK, Byun JY, Park JA, Kim YY, Lee YJ, Oh JI, Jang SY, Kim YH, Song YW,
Son J, Suh KH, Lee YM, Lee EB. HM71224, a novel Bruton's tyrosine kinase
inhibitor, suppresses B cell and monocyte activation and ameliorates arthritis in
a mouse model: a potential drug for rheumatoid arthritis. Arthritis Res Ther.
2016 Apr 18;18:91. doi: 10.1186/s13075-016-0988-z. PubMed PMID: 27090981; PubMed
Central PMCID: PMC4835877.