| CAS NO: | 330786-25-9 |
| Cas No. | 330786-25-9 |
| 别名 | 4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶 |
| Canonical SMILES | NC1=NC=NC2=C1C(C3=CC=C(OC4=CC=CC=C4)C=C3)=NN2C5CCCC5 |
| 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) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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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