PCI 29732

SKU: orb1302940

Description

PCI 29732

Research Area

Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 330786-25-9
• MW: 371.43
• Purity: 99.81%
• Formula: C₂₂H₂₁N₅O
• SMILES: Nc1ncnc2n(nc(-c3ccc(Oc4ccccc4)cc3)c12)C1CCCC1
• Target: BTK,BCRP
• Solubility: DMSO:55 mg/mL (148.08 mM)

Bioactivity

• Target IC50:
  BTK:8.2 nM
• In Vitro:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Breast cancer resistance protein, cytotoxicity, ABCG2, BTK, Btk, B-cell, BCR, BCRP, Bruton tyrosine kinase, Itk, inhibit, PCI 29732, PCI29732, PCI-29732, oral, Inhibitor, reversible

Compound Identifiers

PubChem CID

22347110