Idelalisib

Name: Idelalisib
Brand: Tocris Bioscience
SKU: 7631

Tocris Bioscience, part of Bio-Techne | Catalog # 7631

COA / SDS

Potent PI 3-Kinase δ isoform inhibitor

Key Product Details

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)
Molecular Weight:	415.42

View Full Technical Details for Idelalisib

Technical Data
Citations

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 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.

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	1.20 mL	2.41 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

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References for Idelalisib

References are publications that support the biological activity of the product.

Hoellenriegel The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood 2011 PMID: 21803855
Lannutti CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood 2011 PMID: 20959606
Poli PIP4Ks impact on PI3K, FOXP3, and UHRF1 signaling and modulate human regulatory T cell proliferation and immunosuppressive activity. Proc.Natl.Acad.Sci.U.S.A. 2021 PMID: 34312224
Herman Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood 2010 PMID: 20522708