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PCI 29732

PCI 29732 是一种有效的可逆BTK 抑制剂，对 BTK、Lck 和 Lyn 的Kiapp 值分别为 8.2、4.6 和 2.5 nM。它通过竞争性结合ABCG2 的 ATP 结合位点来抑制ABCG2的功能。

CAS号

330786-25-9

分子式

C22H21N5O

主要靶点

Others|BCRP|BTK

仅限科研使用

Cat No : CM08758

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Synonyms

PCI29732|PCI-29732

验证数据展示

  • CAS No.: 330786-25-9

    PCI 29732
    CAS#: 330786-25-9

产品信息

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

CAS号 330786-25-9
分子式 C22H21N5O
主要靶点 Others|BCRP|BTK
主要通路 离子通道|蛋白酪氨酸激酶|其他|血管生成
分子量 371.44
纯度 99.79%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 PCI29732|PCI-29732

靶点活性

BTK:8.2 nM

体外活性

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.

溶解度

DMSO:>53 mg/mL

参考文献

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.

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