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Chemical Structure| 1353552-97-2 Chemical Structure| 1353552-97-2

Structure of Poseltinib
CAS No.: 1353552-97-2

Chemical Structure| 1353552-97-2

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Poseltinib is a tyrosine kinase inhibitor of Bruton's tyrosine kinase (BTK).

Synonyms: HM71224; LY3337641

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Product Details of Poseltinib

CAS No. :1353552-97-2
Formula : C26H26N6O3
M.W : 470.52
SMILES Code : C=CC(NC1=CC=CC(OC2=C(OC=C3)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O
Synonyms :
HM71224; LY3337641
MDL No. :MFCD31729279
InChI Key :LZMJNVRJMFMYQS-UHFFFAOYSA-N
Pubchem ID :56644522

Safety of Poseltinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of Poseltinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human peripheral blood mononuclear cells (PBMCs) 30 µM 2 hours To evaluate the impact of poseltinib on BTK/PLC and AKT signaling pathways. Results showed that poseltinib significantly inhibited phosphorylation of BTK, AKT, and PLCγ2 in anti-IgM + CD40L stimulated B cells. Sci Rep. 2021 Sep 21;11(1):18671
CD4+ T cells, CD8+ T cells, and NK cells (IL-2 stimulated) 30 µM 2, 5, 15, 60 minutes To evaluate the impact of poseltinib on T cell and NK cell signaling pathways. Results showed that poseltinib inhibited IL-2-stimulated phosphorylation of STAT5 (Y694). Sci Rep. 2021 Sep 21;11(1):18671
B cells (anti-IgM + CD40L stimulated) 30 µM 2, 5, 15, 60 minutes To evaluate the impact of poseltinib on B cell signaling pathways. Results showed that poseltinib significantly inhibited phosphorylation of BTK (Y223), AKT (S473), and PLCγ2 (Y759). Sci Rep. 2021 Sep 21;11(1):18671

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Lewis rats Collagen-induced arthritis (CIA) model Oral 0.3, 1, 3 mg/kg Once daily for 9 consecutive days To evaluate the effect of poseltinib on arthritis severity in CIA model rats. Results showed that 3 mg/kg poseltinib significantly improved arthritis scores and histopathological indices, reducing bone erosion and synovitis. Sci Rep. 2021 Sep 21;11(1):18671

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.63mL

2.13mL

1.06mL

21.25mL

4.25mL

2.13mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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