TG100-115产品描述：TG100-115 是一种选择性的 PI3Kγ/PI3Kδ 抑制剂，IC₅₀ 分别为 83 和 235 nM。
TG100-115产品描述：TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC₅₀s of 83 ａnd 235 nM, respectively.IC50 & Target: IC50: 83 nM （PI3Kγ）, 235 nM （PI3Kδ）^[1]In Vitro: TG100-115 inhibits PI3Kγ ａnd PI3Kδ with IC₅₀s of 83 ａnd 235 nM, respectively, whereas both PI3Kα ａnd PI3Kβ are relatively unaffected （IC₅₀ values >1 μM）. As a gauge of general specificity, TG100-115 is also assayed against a 133 protein kinase panel, of which are inhibited at IC₅₀ values <1 μM. TG100-115 potently inhibits edema ａnd inflammation in response to multiple mediators known to participate in myocardial infarction, including vascular endothelial growth factor ａnd platelet-activating factor; by contrast, endothelial cell mitogenesis, a repair process important to tissue survival after ischemic damage^[1]. In Vivo: To correlate these in vivo responses with the molecular target of interest, PI3K pathway signaling is monitored through western blot analyses of Akt phosphorylation （a PI3K-mediated event）. VEGF injection i.v. in mice induces a rapid Akt phosphorylation readily detectable in lung lysates, pretreatment with TG100-115 blocks this response. Blockade is seen with TG100-115 doses as low as 0.5 mg/kg ａnd persists over a period of several hours. In initial dose-ranging studies, generally equivalent responses are observed using TG100-115 doses of 0.5-10 mg/kg, ａnd we therefore elected to conduct a statistically powered test at the lowest dose. Animals dosed with TG100-115 as a single 0.5 mg/kg i.v. bolus 30 min after reperfusion developed smaller infarcts vs. vehicle-treated controls. Measuring infarct area as percent of total LV ischemic area, infarct size is reduced by 35% （P=0.04）. Viable tissue within the ischemic zone is increased by 37% （P=0.04）, directly demonstrating the cardioprotective effect of PI3Kγ/δ inhibition^[1].

研究领域：Membrane Transporter/Ion Channel

靶点：Calcium Channel

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MWt:346.34

Formula:C18H14N6O2

SMILES:NC1=C（C（N=C2C3=CC（O）=CC=C3）=NC（N）=N1）N=C2C4=CC（O）=CC=C4

Research_Area:Cardiovascular Disease;Cancer



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