ChemicalBook CAS DataBase List 1353552-97-2

1353552-97-2

Name	Poseltinib
CAS	1353552-97-2
Molecular Formula	C26H26N6O3
MDL Number	MFCD31729279
Molecular Weight	470.52
MOL File	1353552-97-2.mol

Chemical Properties

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

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

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