Poseltinib

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].

Product Specifications

CAS Number

[1353552-97-2]

Product Name Alternative

HM71224; LY3337641

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

BMX Kinase; Btk; Toll-like Receptor (TLR)

Type

Reference compound

Related Pathways

Immunology/Inflammation; Protein Tyrosine Kinase/RTK

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/poseltinib.html

Concentration

10mM

Purity

98.08

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C=C)NC1=CC=CC(OC2=C(OC=C3)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1

Molecular Formula

C26H26N6O3

Molecular Weight

470.52

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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. |[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.