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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)
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.
| 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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Product Datasheets for Idelalisib
References for Idelalisib
References are publications that support the biological activity of the product.
Herman et al (2010) Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood 116 2078 PMID: 20522708
Lannutti et al (2011) CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood 117 591 PMID: 20959606
Poli et al (2021) 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. 118 e2010053118 PMID: 34312224
Hoellenriegel et al (2011) The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood 118 3603 PMID: 21803855
If you know of a relevant reference for Idelalisib, please let us know.
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Keywords: Idelalisib, Idelalisib supplier, potent, selective, PI, 3-Kinase, delta, isoform, inhibitor, chronic, lymphocytic, leukemia, cell, permeable, orally, biovavailable, PI3K, 7631, Tocris Bioscience
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