A PI3Kγ and PI3Kδ inhibitor
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TG 100-115

Item No. 10010512

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3,3’-(2,4-diamino-6,7-pteridinediyl)bis-phenol
CAS Number
677297-51-7
Molecular Formula
C18H14N6O2
Formula Weight
346.3
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:(PBS pH 7.2) (1:3): 0.25 mg/ml
λmax
272, 392 nm
SMILES
NC1=C2C(N=C(C3=CC(O)=CC=C3)C(C4=CC=CC(O)=C4)=N2)=NC(N)=N1
InChi Code
InChI=1S/C18H14N6O2/c19-16-15-17(24-18(20)23-16)22-14(10-4-2-6-12(26)8-10)13(21-15)9-3-1-5-11(25)7-9/h1-8,25-26H,(H4,19,20,22,23,24)
InChi Key
UJIAQDJKSXQLIT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

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    10 mg

    $193

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    50 mg

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    Product Description

    TG 100-115 is an inhibitor of PI3Kγ and PI3Kδ (IC50s = 0.083 and 0.235 µM, respectively).1 It is selective for PI3Kγ and PI3Kδ over PI3Kα and PI3Kβ (IC50s = 1.3 and 1.2 µM) and a panel of 140 additional kinases but does inhibit eight kinases in the panel. TG 100-115 also inhibits the kinase activity of transient receptor potential melastatin 7 (TRPM7) with an IC50 value of 1.07 µM.2 TG 100-115 (50 µM) inhibits the migration and invasion of MDA-MB-231 breast cancer cells. It prevents intradermal edema induced by VEGF or histamine and hind paw edema and leukocyte infiltration induced by platelet-activating factor (PAF) or dextran in rats when administered at doses of 1 and 5 mg/kg, respectively.3 TG 100-115 (0.5 mg/kg) decreases infarct size as a percentage of the area at risk in a porcine model of myocardial infarction induced by coronary artery occlusion. It also decreases methacholine-induced airway resistance in an ovalbumin-sensitized mouse model of asthma.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Palanki, M.S.S., Dneprovskaia, E., Doukas, J., et al. Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction. J. Med. Chem. 50, 4279-4294 (2007).

    2. Doukas, J., Wrasidlo, W., Noronha, G., et al. Phosphoinositide 3-kinase γ/δ inhibition limits infarct size after myocardial ischemia/reperfusion injury. Proc. Natl. Acad. Sci. USA 103(52), 19866-19871 (2006).

    3. Doukas, J., Eide, L., Stebbins, K., et al. Aerosolized phosphoinositide 3-kinase gamma/delta inhibitor TG100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease. J. Pharmacol. Exp. Ther. 328(3), 758-765 (2009).