產品屬性：
產品名稱 | PCI 29732 |
規格 | Free Sample (0.1-0.5 mg)、10mM*1mL in DMSO、2mg、5mg、10mg、50mg、100mg、200mg500mg、 |
貨號 | EY-01Y17120 |
Cas No.: 330786-25-9
別名: N/A
化學名: N/A
分子式: C22H21N5O
分子量: 371.44
溶解度: DMSO: ≥ 53 mg/mL (142.69 mM); Ethanol: 10 mg/mL (26.92 mM)
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
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.
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