Idelalisib

Idelalisib

Catalog Number:
CR04341327TOK
Mfr. No.:
TOK-I044
Price:
$161
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      • Overview
        • Idelalisib is the free base version of the compound. It is a small molecule inhibitor of phosphoinositide 3-kinase. It also inhibits other class I P13K enzymes. It also inhibits several signaling pathways, including B-cell receptor signaling.

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          Background

          Idelalisib blocks the delta isoform of the enzyme phosphoinositide 3-kinase signaling, P110δ . The result is decreased phosphorylation of Akt and other effectors. By blocking ongcogenic signaling, the compound has utility for B-cell malignancies.

      • Properties
        • CAS Number
          870281-82-6
          Molecular Formula
          C22H18FN7O
          Molecular Weight
          415.42 g/mol
          Appearance
          Pale yellow to white solid powder
          Solubility
          DMSO (≥59.7 mg/ml)
          Other Properties
          Source: Synthetic
          Purity Level: ≥99% (by HPLC)
          Storage
          -20°C

          * For research use only

      • Applications
        • Application Description
          Cancer Applications: Cytotoxicity p110δ-positive multiple myeloma cells was induced by Idelalisib, but was non toxic to healthy PBMCs. The compound blocked in vitro capillary-like tube formation (angiogenesis). A hallmark of autophagy is LC3-II, and Idelalisib was also found to induce LC3-II (Ikeda et al, 2010).In cell-based assays with B-cell tumor lines and primary cells, Idelalisib had 240- to 2500-fold selectivity for P110δ over the other class I P13K isoforms. In SU-DHL-5, WSU-NHL, and CCRF-SB tumor cell lines, exposure to Idelalisib induced apoptosis, reflected in a 3- to 5-fold increase in annexin V staining. By blocking oncogenic signaling, the compound has utility for B-cell malignancies (Lannutti et al, 2011).

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