CAS NO: | 677297-51-7 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | TG100-115 is a selectivePI3Kγ/PI3Kδinhibitor withIC50s of 83 and 235 nM, respectively. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | TG100-115 inhibits PI3Kγ and PI3Kδ with IC50s of 83 and 235 nM, respectively, whereas both PI3Kα and PI3Kβ are relatively unaffected (IC50values >1 μM). As a gauge of general specificity, TG100-115 is also assayed against a 133 protein kinase panel, none of which are inhibited at IC50values<1 μm. tg100-115 potently inhibits edema and inflammation in response to multiple mediators known participate myocardial infarction, including vascular endothelial growth factor platelet-activating factor; by contrast, cell mitogenesis, a repair process important tissue survival after ischemic damage[1]. | ||||||||||||||||
体内研究 (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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 346.34 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C18H14N6O2 | ||||||||||||||||
CAS 号 | 677297-51-7 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(96.23 mM;ultrasonic and warming and adjust pH to 2 with HCl and heat to 60℃) 配制储备液
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以下溶剂前显示的百
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