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PCI 29732

Catalog No. T4337 CAS 330786-25-9

Synonyms: PCI-29732, PCI29732

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, CAS 330786-25-9

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Purity: 98%

Biological Description

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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	PCI-29732, PCI29732
Molecular Weight	371.444
Formula	C22H21N5O
CAS No.	330786-25-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: >53 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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：

Anti-Cancer Compound Library Inhibitor Library Immuno-Oncology Compound Library Immunology/Inflammation Compound Library Covalent Inhibitor Library Kinase Inhibitor Library Angiogenesis related Compound Library Bioactive Compound Library Tyrosine Kinase Inhibitor Library

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Related compounds with same targets

Ko 143 6,8-Diprenylnaringenin YHO-13177 PCI 29732 Triclabendazole sulfoxide KS176 Brevianamide F Elacridar

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Keywords

PCI 29732 330786-25-9 蛋白酪氨酸激酶离子通道其他血管生成 BCRP BTK Others cytotoxicity Bruton tyrosine kinase Inhibitor Btk ABCG2 reversible PCI29732 BCR inhibit B-cell oral Breast cancer resistance protein PCI-29732 inhibitor

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