CAS NO: | 35943-35-2 |
生物活性 | Triciribine is aDNA synthesisinhibitor, also inhibitsAktandHIV-1/2withIC50of 130 nM, and 0.02-0.46 μM, respectively. | ||||||||||||||||
IC50& Target[1][2][3]
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体外研究 (In Vitro) | The nucleoside analog Triciribine (TCN) is a purine analog which is initially shown to inhibit DNA synthesis. Triciribine selectively inhibits the phosphorylation and activation of all three Akt isoforms. At a concentration of 10 μM Triciribine Akt phosphorylation is inhibited at both Thr308 and Ser473. Triciribine effectively inhibits the phosphorylation and consequently the catalytic activity of Akt in PC-3 cells[1]. The Akt inhibitor Triciribine (TCN) does not effectively inhibit the human cell line U87MG but inhibits other astrocytoma cell lines in a grade-dependent manner. The WHO II K1861-10 line is incompletely inhibited (69% maximum inhibition) with a GI50value of 1.7 μM for Triciribine. Triciribine exhibits maximum growth inhibition around 1-10 μM and inhibits phosphorylation of Akt, as well as downstream p70S6K, to basal levels at 100 μM (IC50=130 nM) in KR158 cells[2]. Triciribine (TCN) is a novel tricyclic compound with known antitumor activity. Using a syncytial plaque assay, Triciribine is active against HIV-1 at 0.01-0.02 μM. Using a microtiter XTT assay, Triciribine is active against a panel of HIV-1 and HIV-2 strains at IC50values ranging from 0.02 to 0.46 μM[3]. | ||||||||||||||||
体内研究 (In Vivo) | Triciribine (TCBN) treatment, administered for 7 days after 14 days of hypoxia until 21 days of hypoxia is reached, reversed the vascular thickening as shown by immunohistochemistry and Western analyses. On the other hand, Rapamycin treatment did not prevent hypoxia-induced pulmonary alveolar haemorrhage and congestion. Triciribine partially inhibits progressive pruning of the vasculature[4]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 320.30 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C13H16N6O4 | ||||||||||||||||
CAS 号 | 35943-35-2 | ||||||||||||||||
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 : 100 mg/mL(312.21 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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