CAL-101 (Idelalisib, GS-1101)

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    CAL-101 (Idelalisib, GS-1101), is a p110δ selective phosphatidylinositol-3-kinase inhibitor in a kinome-wide screen using purified enzymes and in cell-based PI3K isoform-specific assays. Phosphatidylinositol-3-kinase p110δ serves as a central integration point for signaling from cell surface receptors known to promote malignant B-cell proliferation and survival. CAL-101 can block constitutive phosphatidylinositol-3-kinase signaling, resulting in reduced phosphorylation of Akt and other downstream effect factors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis. These effects have been observed across a broad range of immature and mature B-cell malignancies. In addition, CAL-101 abrogated protection from spontaneous apoptosis induced by B cell–activating factors CD40L, TNF-α, and fibronectin.
- Properties
  - Alternative Name
    
    CAL-101,CAL101,Idelalisib,GS-1101,GS1101; 5-fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)propyl]quinazolin-4-one
    
    CAS Number
    
    870281-82-6
    
    Molecular Formula
    
    C22H18FN7O
    
    Molecular Weight
    
    415.43
    
    Appearance
    
    A solid
    
    Purity
    
    99.12%
    
    Solubility
    
    insoluble in H2O; ≥2.1 mg/mL in EtOH with gentle warming and ultrasonic; ≥80.2 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Graeme F. Murray, Daniel Guest, et al. "Single cell biomass tracking allows identification and isolation of rare targeted therapy-resistant DLBCL cells within a mixed population." Analyst. 2021 Feb 21;146(4):1157-1162. PMID:33426547
    2. Julia C Gutjahr, Elisabeth Bayer, et al. "CD44 Engagement Enhances Acute Myeloid Leukemia Cell Adhesion To The Bone Marrow Microenvironment By Increasing VLA-4 Avidity." Haematologica. 2020 Jul 2;haematol.2019.231944. PMID:32616529
    3. Wu W, Zhou G, et al. "PI3Kδ as a Novel Therapeutic Target in Pathological Angiogenesis." Diabetes. 2020;db190713. PMID:31915155
    4. Xin T, Han H, et al. "Idelalisib inhibits vitreous-induced Akt activation and proliferation of retinal pigment epithelial cells from epiretinal membranes." Exp Eye Res. 2019 Nov 28:107884. PMID:31786159
    5. Han H, Chen N, et al. "Phosphoinositide-3-kinase δ inactivation prevents vitreous-induced activation of AKT/MDM2/p53 and migration of retinal pigment epithelial cells." J Biol Chem. 2019 Aug 29. pii: jbc.RA119.010130. PMID:31467081
    6. Yaya Chu, Sanghoon Lee, et al. " Ibrutinib significantly inhibited Bruton’s tyrosine kinase (BTK) phosphorylation,in-vitro proliferation and enhanced overall survival in a preclinical Burkitt lymphoma (BL) model." OncoImmunology.11 Oct 2018.
    7. Wensveen FM, Slinger E, et al. "Antigen-affinity controls pre-germinal centser B cell selection by promoting Mcl-1 induction through BAFF receptor signaling." Sci Rep. 2016 Oct 20;6:35673. PMID:27762293