7224933

Tocris Bioscience™ Idelalisib

Potent PI 3-Kinase δ isoform inhibitor

Manufacturer: Fischer Scientific

CAS Number: 870281-82-6

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Chemical Name or Material

5-Fluoro-3-phenyl-2-[(1 S)-1-(9 H-purin-6-ylamino)propyl]-4(3 H)-quinazolinone

Target

PI 3-Kinase Inhibitors

Purity

98%

CAS

870281-82-6

Molecular Formula

C22H18FN7O

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Description

  • Idelalisib is a potent PI 3-Kinase δ inhibitor (IC50 = 2.5 nM for p110δ); it exhibits >40-fold selectivity for the δ isoform over other PI 3-K class I enzymes (IC50s = 89, 565, and 820 nM for p110γ, p110β, and p110α respectively)
  • Idelalisib blocks constitutive PI 3-K signaling in malignant B-cell lines and primary patient tumor cells
  • Idelalisib inhibits chronic lymphocytic leukemia cell chemotaxis and downregulates chemokine secretion triggered by B-cell receptor signaling in stromal cocultures
  • Idelalisib lacks significant cytotoxicity toward natural killer (NK) cells
  • Idelalisib also decreases production of inflammatory cytokines, including TNF-γ, CD40L, and IL-6 by T cells and IFN-γ by NK cells
  • Idelalisib is cell-permeable and orally bioavailable.

SAFETY INFORMATION

  • Recommended Storage : Store at -20°C