| Identification | Back Directory | [Name]
Poseltinib | [CAS]
1353552-97-2 | [Synonyms]
LY-3337641)
Poseltinib (HM-71224
2-Propenamide, N-[3-[[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]furo[3,2-d]pyrimidin-4-yl]oxy]phenyl]- | [Molecular Formula]
C26H26N6O3 | [MDL Number]
MFCD31729279 | [MOL File]
1353552-97-2.mol | [Molecular Weight]
470.52 |
| Chemical Properties | Back Directory | [density ]
1.316±0.06 g/cm3(Predicted) | [solubility ]
DMSO:100.0(Max Conc. mg/mL);212.53(Max Conc. mM) | [form ]
Solid | [pka]
12.85±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC50 of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis[1][2][3]. | [in vivo]
Poseltinib (3,-30 mg/kg, p.o, once a day, from 18 to 40 weeks) reduces the overactivity of B cells by inhibiting BTK, alleviating the development of systemic lupus erythematosus (SLE) and lupus nephritis (LN)[1].
Poseltinib (1-30 mg/kg p.o, once a day for 2 weeks) improves experimental arthritis in mice [2].
| Animal Model: | MRL/lpr mice and NZB/W F1 mice models[1] | | Dosage: | 3-30 mg/kg | | Administration: | p.o | | Result: | Decreased the spleen weights and prevented skin lesion progression.
Ameliorated renal injury and inflammation and improved the survival rate.
|
| Animal Model: | Collagen-induced arthritis (CIA) mouse model[2] | | Dosage: | 1-30 mg/kg | | Administration: | p.o | | Result: | Reduced the serum IL-6, circulating anti-collagen antibodies and total IgG levels.
Reduced erosive bone changes and prevented bone loss.
|
| [IC 50]
TLRs | [References]
[1] Kim YY, et al. HM71224, a selective Bruton's tyrosine kinase inhibitor, attenuates the development of murine lupus. Arthritis Res Ther. 2017 Sep 26;19(1):211. DOI:10.1186/s13075-017-1402-1
[2] Park JK, et al. 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
[3] Byun JY, et al. Target modulation and pharmacokinetics/pharmacodynamics translation of the BTK inhibitor poseltinib for model-informed phase II dose selection. Sci Rep. 2021 Sep 21;11(1):18671. DOI:10.1038/s41598-021-98255-7 |
|
| Company Name: |
Struchem Co., Ltd.
|
| Tel: |
0512-63009836 18994340901 |
| Website: |
www.beidapharma.com |
|