Idelalisib

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Description: Potent PI 3-Kinase δ isoform inhibitor
Chemical Name: 5-Fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazolinone
Purity: ≥98% (HPLC)
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Biological Activity for Idelalisib

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.

Compound Libraries for Idelalisib

Idelalisib is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Idelalisib

M. Wt 415.42
Formula C22H18FN7O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 870281-82-6
PubChem ID 11625818
InChI Key IFSDAJWBUCMOAH-HNNXBMFYSA-N
Smiles [C@H](NC1=C2C(N=CN2)=NC=N1)(CC)C=3N(C(=O)C=4C(N3)=CC=CC4F)C5=CC=CC=C5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Idelalisib

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.54 100
ethanol 4.15 10

Preparing Stock Solutions for Idelalisib

The following data is based on the product molecular weight 415.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.41 mL 12.04 mL 24.07 mL
5 mM 0.48 mL 2.41 mL 4.81 mL
10 mM 0.24 mL 1.2 mL 2.41 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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Citations for Idelalisib

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