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Chemical Structure| 330786-25-9 Chemical Structure| 330786-25-9

Structure of PCI 29732
CAS No.: 330786-25-9

Chemical Structure| 330786-25-9

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PCI 29732 serves as a highly effective, orally bioavailable, and reversible inhibitor of BTK, displaying Kiapp values of 8.2 nM for BTK, 4.6 nM for Lck, and 2.5 nM for Lyn.

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Product Details of PCI 29732

CAS No. :330786-25-9
Formula : C22H21N5O
M.W : 371.44
SMILES Code : NC1=NC=NC2=C1C(C3=CC=C(OC4=CC=CC=C4)C=C3)=NN2C5CCCC5
MDL No. :MFCD25976874

Safety of PCI 29732

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PCI 29732

RTK

Isoform Comparison

Biological Activity

Description
PCI 29732 serves as a highly effective, orally bioavailable, and reversible inhibitor of BTK, displaying Kiapp values of 8.2 nM for BTK, 4.6 nM for Lck, and 2.5 nM for Lyn. Its inhibitory effect on Itk, another member of the Tec family kinases, is relatively modest. Moreover, PCI 29732 disrupts the activity of ABCG2 by competitively attaching to its ATP-binding site[1].[2].

In Vitro:

Cell Line
Concentration Treated Time Description References
RL B cells 978-1233 nM 2 hours Evaluate the effect of PCI-29732 on LFA-1/ICAM-1 adhesion, results showed PCI-29732 inhibited adhesion with IC50s of 978-1233 nM PMC4512518
Ramos B cells 319 nM 30 minutes Evaluate the effect of PCI-29732 on BCR-mediated calcium flux, results showed PCI-29732 inhibited calcium flux with an IC50 of ~300 nM PMC4512518
Human peripheral B cells 1 μM 1 hour Comparison of the reversible Btk inhibitor PCI-29732 to the irreversible Btk inhibitor PCI-32765 on the transcriptional response of six genes induced by BCR stimulation. PCI-29732 did not affect BCR signaling after washout. PMC2919935

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.92mL

5.38mL

2.69mL

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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