PCI-29732

PCI-29732

CAT N°: 29036
Price:

From 48.00 40.80

PCI-29732 is a multi-kinase inhibitor.{45563} It inhibits the Tec family kinase BTK and the Src family kinases LCK and LYN (Kis = 8.2, 4.6, and 2.5 nM, respectively), as well as the activity of three receptor tyrosine kinases and seven non-receptor tyrosine kinases by greater than 90% in a panel of over 100 kinases at 10 µM. PCI-29732 inhibits calcium flux in Ramos B cells and phosphorylation of phospholipase C?1 (PLC?1) with IC50 values of 0.53 and 0.33 µM, respectively. It is cytotoxic to S1-MI-80, H460/MX20, and KBv200 cancer cells overexpressing the ATP-binding cassette transporter (IC50s = 7.8, 6.3, and 6.02 µM, respectively).{45564} PCI-29732 (20 mg/kg), in combination with the DNA topoisomerase I inhibitor topotecan (Item No. 14129), reduces tumor growth in an H460/MX20 mouse xenograft model.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
  • Correlated keywords
    • PCI29732 multikinase nonreceptor PLC C?1 S1MI80 H-460 MX-20 KBv-200 MI80 S1MI ATPbinding
  • Product Overview:
    PCI-29732 is a multi-kinase inhibitor.{45563} It inhibits the Tec family kinase BTK and the Src family kinases LCK and LYN (Kis = 8.2, 4.6, and 2.5 nM, respectively), as well as the activity of three receptor tyrosine kinases and seven non-receptor tyrosine kinases by greater than 90% in a panel of over 100 kinases at 10 µM. PCI-29732 inhibits calcium flux in Ramos B cells and phosphorylation of phospholipase C?1 (PLC?1) with IC50 values of 0.53 and 0.33 µM, respectively. It is cytotoxic to S1-MI-80, H460/MX20, and KBv200 cancer cells overexpressing the ATP-binding cassette transporter (IC50s = 7.8, 6.3, and 6.02 µM, respectively).{45564} PCI-29732 (20 mg/kg), in combination with the DNA topoisomerase I inhibitor topotecan (Item No. 14129), reduces tumor growth in an H460/MX20 mouse xenograft model.

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