Idelalisib | Selective PI3Kδ Inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 10 mg | $60.00 | ||
| 50 mg | $150.00 |
Idelalisib (CAS 870281-82-6) is a potent (IC50 = 2.5nM) and selective (IC50’s: PI3Ka = 820nM, PI3Kb = 565nM, PI3Kg = 89nM) PI3Kd inhibitor.1,2 Useful clinical agent for the treatment of various blood cancers. Idelalisib attenuates regulatory T cells (Treg) but not conventional T cells (Tconv) resulting in a significant increase in tumor-infiltrating antigen-specific CD8 T cells in a murine lung cancer model.3 Conversely, systemic PI3Kd inactivation antagonized anti-CTLA-4 and anti-PD-L1 treatment.4 Others have found that Idelalisib minimally influenced rituximab- and obinutuzumab-mediated Ab-dependent cellular cytotoxicity in human lymphoma cells.5
References/Citations:
1) Herman et al. (2010), Phosphatidylinositol 2-kinase-d inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals; Blood 116 2078
2) Lannutti et al. (2011), CAL-101, a p110d selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability; Blood 117 591
3) Ahmad et al. (2017), Differential PI3Kd Signaling in CD4+ T-cell Subsets Enables Selective Targeting of T Regulatory Cells to Enhance Cancer Immunotherapy; Cancer Res. 77 1892
4) Lim et al. (2018), Phosphoinositide 3-kinase d inhibition promotes antitumor responses but antagonizes checkpoint inhibitors; JCI Insight 3 e120626
5) Palazzo et al. (2018), The PI3Kd-Selective Inhibitor Idelalisib Minimally Interferes with Immune Effector Function Mediated by Rituximab or Obinutuzumab and Significantly Augment B Cell Depletion In Vivo; J.Immunol. 200 2304
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
Idelalisib (CAS 870281-82-6) is a potent (IC50 = 2.5nM) and selective (IC50’s: PI3Ka = 820nM, PI3Kb = 565nM, PI3Kg = 89nM) PI3Kd inhibitor.1,2 Useful clinical agent for the treatment of various blood cancers. Idelalisib attenuates regulatory T cells (Treg) but not conventional T cells (Tconv) resulting in a significant increase in tumor-infiltrating antigen-specific CD8 T cells in a murine lung cancer model.3 Conversely, systemic PI3Kd inactivation antagonized anti-CTLA-4 and anti-PD-L1 treatment.4 Others have found that Idelalisib minimally influenced rituximab- and obinutuzumab-mediated Ab-dependent cellular cytotoxicity in human lymphoma cells.5
References/Citations:
1) Herman et al. (2010), Phosphatidylinositol 2-kinase-d inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals; Blood 116 2078
2) Lannutti et al. (2011), CAL-101, a p110d selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability; Blood 117 591
3) Ahmad et al. (2017), Differential PI3Kd Signaling in CD4+ T-cell Subsets Enables Selective Targeting of T Regulatory Cells to Enhance Cancer Immunotherapy; Cancer Res. 77 1892
4) Lim et al. (2018), Phosphoinositide 3-kinase d inhibition promotes antitumor responses but antagonizes checkpoint inhibitors; JCI Insight 3 e120626
5) Palazzo et al. (2018), The PI3Kd-Selective Inhibitor Idelalisib Minimally Interferes with Immune Effector Function Mediated by Rituximab or Obinutuzumab and Significantly Augment B Cell Depletion In Vivo; J.Immunol. 200 2304
Related products
-
Zileuton | 5-LO inhibitor
From $32.00CAS:111406-87-2Catalog Number:10-1098Activity:5-LO inhibitorChemical Name:N-(1-Benzo[b]thien-2-ylethyl)-N-hydroxyureaMolecular Weight:236.29Molecular Formula:C11H12N2O2SSolubility:Soluble in DMSO (up to 25 mg/ml).Physical Properties:White solidPurity:>98%
NMR (Conforms)Storage Temperature:-20°CStability:Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.Shipping Code:RT -
Na Valproate | HDAC inhibitor
$40.00CAS:1069-66-5Catalog Number:10-1009Activity:HDAC inhibitorChemical Name:2-Propylpentanoic acid NaMolecular Weight:166.2Molecular Formula:C8H15O2·NaSolubility:Soluble in Water (up to 50 mg/ml).Physical Properties:White solidPurity:98% by TLC
NMR (Conforms)Storage Temperature:-20°CStability:Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20°C for up to 3 monthsShipping Code:RT -
Sunitinib malate | VEGFR, PDGFR kinase inhibitor
From $60.00CAS:341031-54-7Catalog Number:10-1078Activity:VEGFR, PDGFR kinase inhibitorAlternate Names:SU-11248Chemical Name:N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide malateMolecular Weight:532.57Molecular Formula:C22H27FN4O4 C4H6O5Solubility:Soluble in DMSO (up to 13 mg/ml).Physical Properties:Orange solidPurity:98% by TLC
NMR (Conforms)Storage Temperature:-20°CStability:Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.Shipping Code:RT
Calculate the molar concentration, mass or volume in a solution.
Concentration × Volume × Molecular Weight = Mass
