PCI-29732

SKU: orb1225284

Description

A selective and irreversible Btk inhibitor with biochemical Ki of 8.2 nM; also inhibits Lck and Lyn with Ki of 4.6 and 2.5 nM.(In Vitro):PCI29732 shows cytotoxicity in different cells. The IC50 values are 7.94 μM for S1, 7.79 μM for S1-MI-80, 6.55 μM for H460, 6.34 μM for H460/MX20, 6.14 μM for KB, 6.02 μM for KBv200, 12.45 μM for HEK293/pcDNA3, 14.58 μM for HEK293-ABCG2-482-R2, and 13.24 μM for HEK293-ABCG2-482-T7 cells.PCI-29732 blocks the transcriptional up-regulation of a panel of B-cell activation genes in human CD20+ B cells stimulated at the B-cell antigen receptor (BCR).(In Vivo):PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 and enhances the anti-tumor efficacy of substrate chemotherapeutic agents.PCI 29732 (20 mg/kg; p.o.; every 3 d × 5 times) enhances the anticancer efficacy of Topotecan in the H460/MX20 cell xenograft nude mice model.

Key Properties

• CAS Number: 330786-25-9
• MW: 371.435
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₁N₅O
• SMILES: NC1=C2C(N(C3CCCC3)N=C2C4=CC=C(OC5=CC=CC=C5)C=C4)=NC=N1
• Target: BTK
• Solubility: DMSO: ≥ 53 mg/mL

Bioactivity

• In Vivo:
  PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 and enhances the anti-tumor efficacy of substrate chemotherapeutic agents. PCI 29732 (20 mg/kg; p.o. ; every 3 d × 5 times) enhances the anticancer efficacy of Topotecan in the H460/MX20 cell xenograft nude mice model. Animal model: 5-6 weeks old athymic nude mice (bearing H460/MX20 cells). Dosage: 20 mg/kg (combination with Topotecan; every 3 d × 5 times, i.p. , 3 mg/kg; topotecan was given 1 h after PCI29732 administration). Administration: p.o. ; every 3 d × 5 times. Result: Significant reductions in tumor weight and volume were observed in the group treated with PCI29732 in combination with Topotecan.
• In Vitro:
  PCI29732 shows cytotoxicity in different cells. The IC50 values are 7.94 μM for S1, 7.79 μM for S1-MI-80, 6.55 μM for H460, 6.34 μM for H460/MX20, 6.14 μM for KB, 6.02 μM for KBv200, 12.45 μM for HEK293/pcDNA3, 14.58 μM for HEK293-ABCG2-482-R2, and 13.24 μM for HEK293-ABCG2-482-T7 cells. PCI-29732 blocks the transcriptional up-regulation of a panel of B-cell activation genes in human CD20+ B cells stimulated at the B-cell antigen receptor (BCR).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PCI29732 | PCI 29732

Quick Database Links

Gene Symbol

BTK