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PCI 29732

Catalog No. T4337   CAS 330786-25-9
Synonyms: PCI29732, PCI-29732

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.

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PCI 29732 Chemical Structure
PCI 29732, CAS 330786-25-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 80.00
10 mg In stock $ 128.00
25 mg In stock $ 252.00
50 mg In stock $ 449.00
100 mg In stock $ 659.00
1 mL * 10 mM (in DMSO) In stock $ 89.00
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Purity: 99.79%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.
Targets&IC50 BTK:8.2 nM
In vitro PCI 29732(compound 1) has a 8.2 nM potency against Btk in a FRET based biochemical enzymology assay. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase, probably due to the difference at the 'gatekeeper” residue. In human CD20+ B cells stimulated at the BCR, PCI-29732 blocked the transcriptional up-regulation of a panel of B-cell activation genes that occurs within 6 h of stimulation. Pulse exposure to the reversible inhibitor PCI-29732 did not result in BCR inhibition.
Synonyms PCI29732, PCI-29732
Molecular Weight 371.43
Formula C22H21N5O
CAS No. 330786-25-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (148.08 mM)

TargetMolReferences and Literature

1. Pan Z, etal. Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. ChemMedChem. 2007 Jan;2(1):58-61. 2. Honigberg LA, etal. 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 Jul 20;107(29):13075-80.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Inhibitor Library Kinase Inhibitor Library Highly Selective Inhibitor Library Membrane Protein-targeted Compound Library Bioactive Compound Library NO PAINS Compound Library Ion Channel Inhibitor Library Immuno-Oncology Compound Library Anti-Cancer Compound Library

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Keywords

PCI 29732 330786-25-9 Angiogenesis Membrane transporter/Ion channel Others Tyrosine Kinase/Adaptors BCRP BTK cytotoxicity PCI29732 Bruton tyrosine kinase Inhibitor Btk ABCG2 reversible BCR inhibit PCI-29732 B-cell oral Breast cancer resistance protein inhibitor

 

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