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    CAL-101 (Idelalisib, GS-1101)
    CAL-101 (Idelalisib, GS-1101)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0104
    CAS #: 870281-82-6Purity ≥98%

    Description: CAL-101 (also named Idelalisib, GS-1101; trade name Zydelig) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; it has 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. 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. Therefore, Idelalisib has potential immunomodulating and antineoplastic activities. In July 2014, the FDA and EMA granted idelalisib approval to treat different types of leukemia.

    References: Blood. 2011 Jan 13;117(2):591-4; Blood. 2010 Sep 23;116(12):2078-88. 


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    Molecular Weight (MW)415.42
    FormulaC22H18FN7O
    CAS No.870281-82-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 83 mg/mL warming (199.79 mM)
    Water:<1 mg/mL (slightly soluble or insoluble)
    Ethanol: 23 mg/mL (55.36 mM)
    Solubility (In vivo)30% PEG 400 (dissolve first)+0.5% Tween 80+5% Propylene glycol: 30 mg/mL
    Chemical Name(S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one
    SynonymGS1101; GS 1101; GS-1101; CAL101; CAL 101; CAL-101; Idelalisib; trade name Zydelig
    SMILES CodeO=C1N(C2=CC=CC=C2)C([[email protected]@H](NC3=C4N=CNC4=NC=N3)CC)=NC5=C1C(F)=CC=C5


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    In Vitro

    Kinase Assay: PI3K assay is preformed on whole-cell lysates from CLL or normal B cells. A PI3K ELISA assay is performed. Briefly, whole-cell extracts are added to a mixture of PI(4,5)P2 substrate and reaction buffer containing adenosine triphosphate (ATP) and allowed to incubate at room temperature. The reaction is stopped by adding PI(3,4,5)P3 detector mixed with EDTA (ethylenediaminetetraacetic acid) and allowed to incubate at room temperature for 1 hour. After this time, the mixture is transferred from each well to a PI3K ELISA plate and allowed to incubate 1 hour. Plates are washed and then incubated with secondary detector for 30 minutes. Plates are washed again, and 3,3′,5,5′-tetramethylbenzidine solution is added for 5 minutes at which time H2SO4 is added to stop all reactions. Plates are read at 450 nm on a Labsystems 96-well plate reader.


    Cell Assay: CLL B cells or healthy volunteer T cells or NK cells; MTT assays are performed to determine cytotoxicity. 1 × 105cells are incubated with CAL-101. MTT reagent is then added, and plates are incubated for an additional 20 hours before washing with protamine sulfate in phosphate-buffered saline. DMSO is added, and absorbance is measured by spectrophotometry at 540 nm in a Labsystems plate reader. Cell viability is also measured at various time points with the use of annexin/PI flow cytometry. Data are analyzed. At least 104 cells are counted for each sample. Results are expressed as the percentage of total positive cells over untreated control. Experiments examining caspase-dependent apoptosis included the addition of 100 μM Z-VAD. Experiments examining survival signals include the addition of 1 μg/mL CD40L, 800 U/mL IL-4, 50 ng/mL BAFF, 20 ng/mL TNF-α, or coculturing on fibronectin or stromal (HS-5 cell line) coated plates. Stromal coculture is done by plating a 75-cm2 flask (80%-100% confluent) per 6-well plate 24 hours before the addition of CLL cells.

    CAL-101 is not sensitive to other PI3K class I subunits including p110α, p110β, and p110γ. CAL-101 specifically blocks FcϵR1 p110δ-mediated CD63 expression with an EC50 of 8 nM in primary basophil. CAL-101 exhibits greater activity in B-cell acute lymphoblastic leukemia (B-ALL) and chronic lymphocytic leukemia (CLL) cells compared with acute myeloid leukemia (AML) and myeloproliferative neoplasm (MPN) cells. CAL-101 produces the reduction in pAktS473, pAktT308, and the downstream target S6 in SU-DHL-5, KARPAS-422 and CCRF-SB cells with EC50 of 0.1 to 1.0 μM. CAL-101 induces selective cytotoxicity in CLL cells independent of IgVH mutational status or interphase cytogenetics, primarily through a caspase-dependent mechanism. CAL-101 induces cytotoxicity preferentially to CLL cells compared with normal B cells, without producing cytotoxicity in other hematopoietic cells, compared to LY294002. CAL-101 lacks direct cytotoxic potential to T cells and nature killer (NK) cells. CAL-101 can inhibit production of inflammatory cytokines, such as IL-6, IL-10, TNF-α, and IFN-γ, and activation-induced cytokines, such as CD40L. CAL-101 also antagonizes CD40L-mediated CLL cell survival. CAL-101 induces an accumulation of cells in G1 and a decrease in the S-phase population in L1236 and L591 cells, which indicates CAL-101 as a novel strategy for the treatment of hodgkin lymphoma (HL).

    In VivoAdministration of GDC-0941 at 75 mg/kg/day displays significant inhibitory effect against established human U87MG glioblastoma xenografts in female NCr athymic mice, with tumor growth inhibition of 83%. Oral administration of GDC-0941 at 150 mg/kg/day inhibits the growth of HER2-amplified, trastuzumab-resistant MDA-MB-361.1 xenografts in mice, and significantly delays the tumor progression, in association with potent induced apoptosis in tumors. GDC-0941 (75 mg/kg/day) treatment for 2 weeks induces ~40% reduction in tumor volume of spontaneous B-cell follicular lymphomas developed in PTEN+/-LKB1+/hypo mice, accompanied by ablation of phosphorylation of Akt, S6K and SGK (serum and glucocorticoid protein kinase) protein kinases.
    Animal modelNOD-SCID-γ-null (NSG) mice well-engrafted with de novo (n = 3) or relapsed (n = 1) childhood Ph-like ALL specimens with JAK2 mutations and/or CRLF2 alterations.
    Formulation & Dosage30 mg/kg/day, 3 days, oral gavage
    References

    [1] Lannutti BJ, et al. Blood, 2011, 117(2), 591-594.[2] Herman SE, et al. Blood, 2010, 116(12), 2078-2088.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    CAL-101 (Idelalisib, GS-1101)

    CAL-101 inhibits PI3Kδ with high selectivity.  2011 Jan 13;117(2):591-4.


    CAL-101 (Idelalisib, GS-1101)

    CAL-101 inhibits PI3K signaling and cellular viability.  2011 Jan 13;117(2):591-4.



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