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Poseltinib

Cat. No. M11431

All AbMole products are for research use only, cannot be used for human consumption.

Poseltinib Structure
Synonym:

HM71224; LY3337641

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Quality Control & Documentation
Biological Activity

Poseltinib is an orally active, selective, irreversible small-molecule Bruton tyrosine kinase (BTK) inhibitor with an IC50 of 1.95 nM and 0.3, 2.3, and 2.4 fold selective action against BMX, TEC, and TXK, respectively. Poseltinib covalently binds to the active site of BTK (cysteine 481 residue) and effectively inhibits B cell receptor (BCR), Fc receptor (FcR), and Toll-like receptor (TLR) mediated signaling.

Chemical Information
Molecular Weight 470.52
Formula C26H26N6O3
CAS Number 1353552-97-2
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Joo-Yun Byun, et al. Sci Rep. Target modulation and pharmacokinetics/pharmacodynamics translation of the BTK inhibitor poseltinib for model-informed phase II dose selection

[2] Mark C Genovese, et al. J Rheumatol. Safety and Efficacy of Poseltinib, Bruton's Tyrosine Kinase Inhibitor, in Patients With Rheumatoid Arthritis: A Randomized, Double-blind, Placebo-controlled, 2-part Phase II Study

Related BTK Products
BIIB129

BIIB129 is a covalent, selective inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier. BIIB129 inhibits the activity of BTK by covalently binding to Cys481 in BTK, thereby affecting the function of B cells and myeloid cells.

UBX-382 

UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling.

GDC-0834 

GDC-0834 is a potent and selective BTK inhibitor.

DD-03-171 

DD-03-171 is a BTK, IKFZ1 and IKFZ3 degrader, the BTK IC50 a value of 5.1 nM.

N-piperidine Ibrutinib hydrochloride 

N-piperidine Ibrutinib hydrochloride is a reversible Ibrutinib derivative.

  Catalog
Abmole Inhibitor Catalog




Keywords: Poseltinib, HM71224; LY3337641 supplier, BTK, inhibitors, activators

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