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    PI-3065
    PI-3065

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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 #: V0149
    CAS #: 955977-50-1Purity ≥98%

    Description: PI-3065 is a novel, potent and selective inhibitor of PI3K (phosphatidylinositol 3-kinase) p110δ inhibitor with potential anticancer activity. It inhibits p110δ with an IC50 of 15 nM, and showed >70-fold selectivity over other PI3K family proteins such as p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM, respectively. 

    References: Nature. 2014 Jun 19;510(7505):407-11. 

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    Molecular Weight (MW)

    506.64

    Formula

    C27H31FN6OS

    CAS No.

    955977-50-1

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 50 mg/mL warming (98.7 mM)

    Water:<1 mg/mL

    Ethanol: <1 mg/mL

    Synonym

    PI-3065; PI3065; PI 3065.

    Chemical Name

    4-(6-((4-(cyclopropylmethyl)piperazin-1-yl)methyl)-2-(5-fluoro-1H-indol-4-yl)thieno[3,2-d]pyrimidin-4-yl)morpholine


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    In Vitro

    Kinase Assay: PI-3065 is a novel, potent and selective inhibitor of PI3K (phosphatidylinositol 3-kinase) p110δ inhibitor with potential anticancer activity. It inhibits p110δ with an IC50 of 15 nM, and showed >70-fold selectivity over other PI3K family proteins such as p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM, respectively. 


    Cell Assay: Proliferation of 4T1 cells is assayed following a 4-h treatment with the indicated p110δ inhibitors, then washing and MTS staining are carried out after 48 h culture. PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ

    In Vivo

    In mouse model, PI-3065 (75 mg/kg, p.o.) also suppresses 4T1 tumor growth and metastasis via inactivation of p110δ. In the LSL.KrasG12D/+; p53R172H/+; PdxCretg/+ (or KPC) model of pancreatic ductal adenocarcinoma, PI-3065 prolongs survival and reduces the incidence of macroscopic metastases and other disease-associated pathologies.

    Animal model

    Female WT BALB/c mice bearing 4T1 tumors

    Formulation & Dosage

    Dissolved in 0.5% methylcellulose with 0.2% Tween 80; 75 mg/kg; Oral administration

    References

    [1] Ali K, et al. Nature. 2014, 510(7505), 407-411.


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

    PI-3065

    Impact of pharmacological inactivation of p110δ on tumour growth and T cell responses. Nature. 2014, 510(7505), 407-411.

    PI-3065

    Characterisation of the p110δ-selective inhibitor PI-3065


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