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受注：045-509-1970 |
技術サポート：tech@selleck.co.jp 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
化学情報
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Synonyms | NSC 154020, VD-0002, vqd-002, TCN | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C13H16N6O4 |
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| 分子量 | 320.3 | CAS No. | 35943-35-2 | |
| Solubility (25°C)* | 体外 | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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生物活性
| 製品説明 | Triciribine (API-2) は、DNA synthesis阻害剤であり、PC3細胞株のAktおよびCEM-SS、H9、H9IIIB、U1細胞のHIV-1もそれぞれ130 nMおよび20 nMのIC50で阻害します。PI3K/PDK1は阻害しません。アデノシンキナーゼを欠損する細胞では5000倍活性が低いです。第1/2相。 |
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| in vitro | Triciribine (API-2) exhibits maximum growth inhibition around 1-10 μM and inhibits phosphorylation of Akt, as well as downstream p70S6K, to basal levels at 100μM (IC50 = 130 nM). It shows particular promise for inhibiting growth in Nf1 and Trp53 mutant astrocytoma cells in a grade-dependent manner. The WHO II K1861-10 line is inhibited, incompletely (69% maximum inhibition), with a GI50 value of 1.7 μM for this compound, whereas higher-grade tumor lines (KR158, KR130, and SF295) are inhibited to a greater extent (>80% maximum inhibition) at lower GI50 values (0.4–1.1 mM). Importantly, it is much less effective at inhibiting primary astrocytes (GI5013.6 mM), suggesting that this inhibitor may show specificity for tumor cells. It inihibits HIV-1with an IC50 of 20 nM. Greater than 90% inhibition is achieved at 0.1μM and complete inhibition of syncytia formation is achieved at 5μM. Associated cell toxicity in the same cell line for Triciribine is 46 μM, resulting in selectivity indices of 2250. It markedly inhibits HIV-1-induced p24 core antigen production, reverse transcriptase, and infectious virus production in a dose-dependent manner using HIV-1 acutedly infected CEM-SS, H9, and persistently infected H9III B and U1 cells. This compound inhibits Akt phosphorylation at Thr308 and Ser473 and Akt activity in the human prostate cancer cell line PC-3. It sensitizes PC-3 cells to TRAIL- and anti-CD95-induced apoptosis, whereas the cells remain resistant to DNA damaging chemotherapeutics. It is highly selective for Akt and does not inhibit the activation of phosphatidylinositol 3-kinase, phosphoinositide-dependent kinase-1, protein kinase C, serum and glucocorticoid-inducible kinase, protein kinase A, signal transducer and activators of transcription 3, extracellular signal-regulated kinase-1/2, or c-Jun NH2-terminal kinase. |
| in vivo | Triciribine (API-2), administered at 1 mg/kg/day i.p., inhibits tumor growth by 90%, 88%, and 80% in nude mice bearing OVCAR3, OVCAR8, and PANC1 tumors, respectively, which overexpress Akt. However, this compound has little effect on the growth of OVCAR5 and COLO357 cells. |
プロトコル(参考用のみ)
| キナーゼアッセイ | Akt Phosphorylation Changes Assay | |
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| Cells are grown to 80%–90% confluency and stimulated for 5–10 minutes with 1–10 ng/mL of epidermal growth factor or platelet derived growth factor (PDGF)–AA with or without 10–20 mM of U0126 or LY-294002. Protein lysates (5–20 μg) are separated by 12%–15% SDS PAGE and analyzed by Western blot for Akt, phosphorylated Akt (phospho-Ser 473), MAPK, and phosphorylated MAPK (p44/42 phospho-Thr202/Tyr204) antibodies (1:1000). | ||
| 細胞アッセイ | 細胞株 | CEM-SS cells |
| 濃度 | 0-500 μM | |
| 反応時間 | 48 hours | |
| 実験の流れ | Triciribine (API-2) is evaluated for cytotoxicity by seeding CEM-SS cells at a density of 1 × 104 cells/well in growth medium, using a 96-well flat-bottom plate. Serial fivefold dilutions of this compound are prepared in growth medium and added to the wells as a second overlay. After a 48-hours incubation at 37 °C, the cells are pulse labeled with [3H]dThd (1 μCi per well, specific activity 20 Ci/mmol) for 6 hours and the cells are harvested to measure total DNA synthesis. | |
| 動物実験 | 動物モデル | OVCAR3, OVCAR8, PANC1, OVCAR5 and COLO357 tumor cells are injected s.c. into 80week-old female nude mice. |
| 投薬量 | 1 mg/kg/day | |
| 投与方法 | Triciribine is administrated through i.p. injection once a day. | |
参考
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カスタマーフィードバック
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, , Oncol Lett, 2016, 11(3):1889-1894.
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Data from [Data independently produced by , , Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2307-2318]
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Data from [Data independently produced by , , Oncotarget, 2016, 7(30):48346-48359]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| βIV spectrin abundancy, cellular distribution and sensitivity to AKT/GSK3 regulation in schizophrenia [ Mol Psychiatry, 2025, 10.1038/s41380-025-02917-1] | PubMed: 39920295 |
| Dual inhibition of AKT and autophagy sensitizes triple negative breast cancer cells to carboplatin [ Transl Oncol, 2025, 58:102434] | PubMed: 40450899 |
| Lamin A/C phosphorylation at serine 22 is a conserved heat shock response to regulate nuclear adaptation during stress [ J Cell Sci, 2023, 136(4)jcs259788] | PubMed: 36695453 |
| Functional restoration of lysosomes and mitochondria through modulation of AKT activity ameliorates senescence [ Exp Gerontol, 2023, 173:112091] | PubMed: 36657533 |
| Regulation of miRNA expression by α4β1 integrin-dependent multiple myeloma cell adhesion [ EJHaem, 2023, 4(3):631-638] | PubMed: 37601846 |
| CREB3L1 promotes tumor growth and metastasis of anaplastic thyroid carcinoma by remodeling the tumor microenvironment [ Mol Cancer, 2022, 21(1):190] | PubMed: 36192735 |
| Disruption of the IL-33-ST2-AKT signaling axis impairs neurodevelopment by inhibiting microglial metabolic adaptation and phagocytic function [ Immunity, 2022, 55(1):159-173.e9] | PubMed: 34982959 |
| DENR controls JAK2 translation to induce PD-L1 expression for tumor immune evasion [ Nat Commun, 2022, 13(1):2059] | PubMed: 35440133 |
| Anionic nanoplastic exposure induces endothelial leakiness [ Nat Commun, 2022, 13(1):4757] | PubMed: 35963861 |
| CRISPR/Cas9 Screens Reveal that Hexokinase 2 Enhances Cancer Stemness and Tumorigenicity by Activating the ACSL4-Fatty Acid β-Oxidation Pathway [ Adv Sci (Weinh), 2022, 9(21):e2105126] | PubMed: 35603967 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。