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ChemicalBook Optimization Suppliers |
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| 化学名: | トリシリビン | | 英語化学名: | API-2 | | 别名: | API-2;6-AMINO-4-METHYL-8-(BETA-D-RIBOFURANOSYL)-4H,8H-PYRROLO[4,3,2-DE]PYRIMIDO[4,5-C]PYRIDAZINE;AKT/PKB SIGNALING INHIBITOR-2;AKT INHIBITOR V;1,5-DIHYDRO-5-METHYL-1-BETA-D-RIBOFURANOSYL-1,4,5,6,8-PENTAAZAACENAPHTHYLEN-3-AMINE;1,4,5,6,8-pentaazaacenaphthylen-3-amine,1,5-dihydro-5-methyl-1-beta-d-ribofura;API-2 (Tricirbine);TRICIRIBINE | | CAS番号: | 35943-35-2 | | 分子式: | C13H16N6O4 | | 分子量: | 320.3 | | EINECS: | | | カテゴリ情報: | Akt;mTOR;Inhibitors;Protein Kinase;PI3K;pharmaceutical | | Mol File: | 35943-35-2.mol |  |
| 融点 | 207 °C (decomp) | | 沸点 | 459.21°C (rough estimate) | | 比重(密度) | 1.2633 (rough estimate) | | 屈折率 | 1.7000 (estimate) | | 貯蔵温度 | Store at RT | | 溶解性 | DMSO: >10mg/mL | | 外見 | powder | | 酸解離定数(Pka) | 12.35±0.70(Predicted) | | 色 | tan | | InChIKey | HOGVTUZUJGHKPL-HTVVRFAVSA-N |
| WGK Germany | 3 | | RTECS 番号 | RY8455000 |
| | トリシリビン Usage And Synthesis |
| 化学的特性 | Off-White Solid | | 使用 | Triciribine is an antitumor tricyclic nucleoside. Triciribine acts as a potent, small-molecule inhibitor of AKT phosphorylation in subjects with solid tumors contining activated AKT. Triciribine is al
so a selective inhibitor of HIV-1 and HIV-2, including strains known to be resistant to AZT or TIBO. | | 使用 | Triciribine hydrate has been used to study the effect of diethyldithiocarbamate (DDC) on matrix metalloproteinase-1 (MMP-1) in hepatic stellate cells1. It has also been used to analyze ADAM 10 activation by (-)-epigallocatechin-3-gallate (EGCG) in N2a cells overexpressing Swedish mutant APP (SweAPP N2a cells)2. | | 使用 | Triciribine is an antitumor tricyclic nucleoside. Triciribine acts as a potent, small-molecule inhibitor of AKT phosphorylation in subjects with solid tumors contining activated AKT. Triciribine is also a selective inhibitor of HIV-1 and HIV-2, including strains known to be resistant to AZT or TIBO. | | 定義 | ChEBI: Triciribine is a nucleoside analogue in which the nucleobase portion is a 1,4,5,6,8-pentaazaacenaphthylene ring system substituted with an amino group at position 3, and a methyl group at position 5 and is bound to the beta-D-ribofuranosyl moiety by an N(1)-glycosidic linkage. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor. | | 生物活性 | Selective inhibitor of Akt (protein kinase B) signaling; displays minimal inhibition of PKC, PKA, SGK and p38 pathways. Inhibits phosphorylation and activation of downstream targets of Akt including Bad, GSK-3 β and AFX. In vitro, induces apoptosis and growth arrest preferentially in human cancer cells with elevated levels of Akt. In mice, potently and selectively inhibits growth of Akt-overexpressing tumors. Inhibits DNA synthesis and displays antiviral activity against HIV-1 and -2. | | Biochem/physiol Actions | Triciribine is a highly selective Akt/PKB inhibitor, that selectively inhibits the cellular phosphorylation/activation of Akt1/2/3. | | 貯蔵 | Store at RT |
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