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PCI 29732
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PCI 29732图片
CAS NO:330786-25-9
规格:98%
分子量:371.44
包装与价格:
包装价格(元)
200mg电议
500mg电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
PCI 29732是不可逆的Btk抑制剂,IC50为8.2 nM。
CAS:330786-25-9
分子式:C22H21N5O
分子量:371.44
纯度:98%
存储:Store at -20°C

Background:

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.IC50 value: 8.2 nM [1]Target: Btk kinasePCI 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 [1].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 [2].




[1]. Pan Z, et al. Discovery of selective irreversible inhibitors for Bruton’s tyrosine kinase. ChemMedChem. 2007 Jan;2(1):58-61. [2]. 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 Jul 20;107(29):13075-80.