Home Protein Tyrosine Kinase BTK inhibitor PCI 29732

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PCI 29732 BTK inhibitor

Cat.No.S6725

PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM.
PCI 29732 BTK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 371.43

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S672501 DMSO]74 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.91%
99.91

Chemical Information, Storage & Stability

Molecular Weight 371.43 Formula

C22H21N5O

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 330786-25-9 -- Storage of Stock Solutions

Synonyms N/A Smiles C1CCC(C1)N2C3=NC=NC(=C3C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)N

Solubility

In vitro
Batch:

DMSO : 74 mg/mL (199.23 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
BTK [1]
(Cell-free assay)
0.5 nM
BLK [1]
(Cell-free assay)
0.5 nM
Bmx [1]
(Cell-free assay)
0.8 nM
EGFR [1]
(Cell-free assay)
5.6 nM
YES [1]
(Cell-free assay)
6.5 nM
ErbB2 [1]
(Cell-free assay)
9.4 nM
ITK [1]
(Cell-free assay)
10.7 nM
JAK3 [1]
(Cell-free assay)
16.1 nM
FRK [1]
(Cell-free assay)
29.2 nM
LCK [1]
(Cell-free assay )
33.2 nM
RET [1]
(Cell-free assay)
36.5 nM
In vitro

PCI-32765 blocks BCR signaling in human peripheral B cells at concentrations that does not affect T cell receptor signaling. In DOHH2 cells, PCI-32765 inhibits autophosphorylation of Btk (IC50, 11 nM), phosphorylation of Btk’s physiological substrate PLCγ(IC50, 29 nM), and phosphorylation of a further downstream kinase, ERK (IC50, 13 nM). PCI-32765 is more than 1,000-fold selective for inhibition of antigen receptor signaling in B cells over T cells, and that only B-cell inhibition is sustained following short duration treatment[1].
In vivo

In mice with collagen-induced arthritis, orally administered PCI-32765 reduces the level of circulating autoantibodies and completely suppresses disease. PCI-32765 also inhibits autoantibody production and the development of kidney disease in the MRL-Fas(lpr) lupus model. The mean terminal plasma half-life of PCI-32765 following oral dosing in mice is 1.7 to 3.1 h[1].
References

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