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    Pilaralisib (XL147; SAR245408)
    Pilaralisib (XL147; SAR245408)

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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 #: V0150
    CAS #: 934526-89-3Purity ≥98%

    Description: Pilaralisib (formerly XL-147; SAR-245408) is a novel, potent, orally bioavailable, ATP-competitive, selective and reversible inhibitor of class I PI3K (phosphatidylinositol 3-kinase) with potential anticancer activity. It inhibits PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, and is less potent against PI3Kβ. Pilaralisib has been  studied for he treatment of various cancers such as lymphoma, solid tumors, glioblastoma, and breast cancer.

    References: Clin Cancer Res. 2014 Jan 1;20(1):233-45. 

    Related CAS #: 956958-53-5 (XL147 analog)

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    Molecular Weight (MW)

    541.02

    Formula

    C25H25ClN6O4S

    CAS No.

    934526-89-3

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 100 mg/mL warming (184.8 mM)

    Water:<1 mg/mL

    Ethanol: <1 mg/mL

    Solubility (In vivo)

    10 mM HCl in sterile water: 0.5mg/mL 

    Synonym & Chemical Name

    XL147; XL 147; XL-147; SAR245408; SAR-245408; SAR 245408; N-(3-{[(3-{[2-chloro-5-(methoxy)phenyl]amino}quinoxalin-2-yl)amino]sulfonyl}phenyl)-2-methylalaninamide


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    In Vitro

    Kinase Assay: Kinase activity for PI3K isoforms is measured as the percentage of ATP consumed following the kinase reaction using luciferase–luciferin-coupled chemiluminescence, with ATP concentrations approximately equal to the Km for each respective kinase. Kinase reactions are initiated by combining test compounds, ATP and kinase in a 20 μL volume. PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ final enzyme concentrations are 0.5, 8, 20, and 2 nM, respectively. Of note, 0.5 μL dimethyl sulfoxide (DMSO) containing varying concentrations of the test compound is mixed with 10 μL enzyme solution (2×concentration). Kinase reactions are initiated by the addition of 10 μL of liver phosphatidylinositol and ATP solution (2×concentration). Assay concentrations for VPS34, ATP, and phosphatidylinositol are 40 nM, 1 μM, and 5 μM, respectively

     

    Cell Assay: Cell proliferation is measured by using MTT or pre-mixed WST-1 reagent. For MTT/WST-1 assays, 10,000 cells/well are seeded in 96-well plates. 24 h after plating, cells (BT474 cells) are treated with DMSO or pilaralisib. After 5 days of treatment, MTT/WST-1 assays are performed. Pilaralisib exhibits cytotoxic activity in Pediatric Preclinical Testing Program (PPTP) cell lines, with a median relative IC50 value of 10.9 mM (range 2.7 mM to 24.5 mM).

    In Vivo

    In BALB/c nu/nu mice, Pilaralisib (100 mg/kg, p.o.) induces tumor growth inhibition for solid glioma xenografts. Pilaralisib is well tolerated, with only 0.7% toxicity rate in the treated groups, similar to that observed for control animals. In athymic female mouse, Pilaralisib (100 mg/kg, p.o.) significantly delays tumor growth without significant drug-related toxicity.

    Animal model

    BALB/c nu/nu mice with glioma xenografts

    Formulation & Dosage

    Dissolved in 10 mM HCl in sterile water; 100 mg/kg; oral administration

    References

    [1] Reynolds CP, et al. Pediatr Blood Cancer. 2013, 60(5), 791-798.[2] Foster P, et al. Mol Cancer Ther. 2015, 14(4), 931-940.

     


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

    Pilaralisib (XL147)

    SAR245408 (XL147) in vitro activity

    Pilaralisib (XL147)

    SAR245408 (XL147) activity in vivo against individual tumor xenografts. Pediatr Blood Cancer. 2013, 60(5), 791-798.


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