PCI29732 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。

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

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.

330786-25-9

C22H21N5O

371.44

PCI29732;PCI-29732

DMSO:>53 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years