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    TG100713
    TG100713

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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 #: V0142
    CAS #: 925705-73-3Purity ≥98%

    Description: TG100713 is a novel and potent pan-PI3K (phosphatidylinositol 3-kinase) inhibitor with potential anti-inflammatory activity. It inhibits PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively. PI3Kγ and PI3Kδ are a pair of pro-inflammatory PI3K isoforms that contribute to the inflammation which causes damages to ischemia tissue upon reperfusion. Phosphoinositide 3-kinases (PI3Ks) are benefit to pro-cell survival roles during tissue iscg the reperfusion phhemia. Therefore, it is possible that selectively inhibiting pro-inflammatory PI3K isoforms durinase could ultimately control overall tissue damage caused by ischemia/reperfusion injuries such as myocardial infarction.

    References:  Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19866-71. 

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    Molecular Weight (MW)

    254.25

    Formula

    C12H10N6

    CAS No.

    925705-73-3

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 2 mg/mL (7.86 mM)

    Water:<1 mg/mL

    Ethanol: <1 mg/mL

    Other info

    Synonym: TG100713; TG-100713; TG 100713

    SMILES Code: OC1=CC=CC(C2=NC3=C(N)N=C(N)N=C3N=C2)=C1

    Chemical Name

    3-(2,4-diaminopteridin-6-yl)phenol


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    In Vitro

    Kinase Assay: PI3K reactions are constructed by using recombinant human kinases, 3 μM ATP, phosphatidylinositol substrate, and cofactors, and reaction progression measured by using a luminescent-based detection system to quantify ATP consumption. Protein kinase assays are performed by using commercial screening services.

     

    Cell Assay: TG 100713 also strongly inhibits EC proliferation. Human umbilical vein EC (HUVEC) plated in 96-well cluster plates (5,000 cells/well) are cultured in assay medium (containing 0.5% serum and 50 ng/ml VEGF) in the presence or absence of test compounds (10 μM), and cell numbers are quantified by XTT assay.

    Modeling studies suggested that the freedom of conformational rotation permitted by ring substituents controls isoform selectivity. Although substituent ring of TG100-115, TG100713, and TG101110 all require energy minima at 30–40°, angles diverge of each compound results in paying differing penalties from this range. TG100-115 displays the greatest barrier to rotation and finally is the most isoform selective, TG100713 has the most conformational flexibility (ring A being almost freely rotatable with maxima ≈5 kcal; 1 kcal = 4.18 kJ), suggesting the least selective, and TG101110 lies an intermediate position (several conformations ≦10 but some >>50 kcal)

    In Vivo

    The minimum structure which satisfies all three requirements is shown in TG100713, which so far has also displayed the best PI3K binding activity. Interestingly, the SAR profiles generating correlate quite well with the results of the initial in vivo screen further supports the involvement of PI3K as a target for inhibiting vascular permeability in related compounds

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    References

    Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19866-71; J Med Chem. 2007 Sep 6;50(18):4279-94.


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

    TG100713

    Inhibition of cell proliferation and signaling. Proc Natl Acad Sci U S A, 2006, 103(52), 19866-19871.


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