TG 100-115

TG 100-115 is an inhibitor of PI3Kgamma and PI3Kdelta (IC50s = 0. and 0. µM, respectively). It is selective for PI3Kgamma and PI3Kdelta over PI3Kalpha and PI3Kbeta (IC50s = 1. and 1. 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. µM. 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. TG 100-115 (0. 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.. Solulibility: DMF: 1 mg/ml: DMSO: 1 mg/ml, DMSO:(PBS pH 7.2) (1:3): 0.25 mg/ml.