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PCI 29732

CAT: 0804-HY-18010-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-18010-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
PCI 29732 is a potent, orally active, reversible BTK inhibitor with Kiapp values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2[1][2].
CAS Number
330786-25-9
UNSPSC
12352005
Hazard Statement
H302-H315-H319-H335
Target
BCRP; Btk
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel; Protein Tyrosine Kinase/RTK
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/PCI-29732.html
Purity
99.86
Solubility
DMSO : ≥ 53 mg/mL|Ethanol : 10 mg/mL (ultrasonic)
Smiles
NC1=NC=NC2=C1C(C3=CC=C(OC4=CC=CC=C4)C=C3)=NN2C5CCCC5
Molecular Formula
C22H21N5O
Molecular Weight
371.44
Precautions
P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501
References & Citations
[1]Pan Z, et al. Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. ChemMedChem. 2007 Jan;2 (1) :58-61.|[2]Ge C, et al. PCI29732, a Bruton's Tyrosine Kinase Inhibitor, Enhanced the Efficacy of Conventional Chemotherapeutic Agents in ABCG2-Overexpressing Cancer Cells. Cell Physiol Biochem. 2018;48 (6) :2302-2317.|[3]Honigberg LA, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010;107 (29) :13075-13080.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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A16262-2PCI 29732 2mg
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A16262-100PCI 29732 100mg
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