CAS:35943-35-2
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Light yellow to brown Solid
Triciribine 是一种 DNA 合成 (DNA synthesis) 抑制剂,也抑制 Akt 和 HIV-1/2。
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TriciribineCAS:35943-35-2
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Light yellow to brown Solid
CAS | 35943-35-2 |
Chinese Name | 曲西立滨 |
English Name | Triciribine |
Synonyms | NSC 154020;VD-0002;vqd-002;TCN;API-2;Tricyclic nucleoside |
Molecular Formula | C13H16N6O4 |
Molecular Weight | 320.3 |
Solubility | Soluble in DMSO |
Purity | ≥98% |
Appearance | Light yellow to brown Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL | MFCD00932413 |
SMILES | OC[C@H]1O[C@H]([C@H](O)[C@@H]1O)N2C3=NC=NC4=C3C(C(N)=NN4C)=C2 |
Target Point | DNA/RNA Synthesis |
Passage | Cell Cycle;DNA Damage/DNA Repair |
Background | Triciribine is a DNA synthesis inhibitor that also inhibits Akt and HIV-1/2. |
Biological Activity | Triciribine 是一种 DNA 合成 (DNA synthesis) 抑制剂,也抑制 Akt 和 HIV-1/2,IC50 分别为 130 nM 和 0.02-0.46 μM。[1-4] |
In Vitro | 核苷类似物Triciribine(TCN)是嘌呤类似物,最初显示其抑制DNA合成。 Triciribine选择性地抑制所有三种Akt同种型的磷酸化和活化。浓度为10μM时,Thr308和Ser473均抑制Triciribine Akt磷酸化。 Triciribine有效抑制Akt在PC-3细胞中的磷酸化和催化活性[1]。 Akt抑制剂Triciribine(TCN)不能有效抑制人细胞系U87MG,但以等级依赖性方式抑制其他星形细胞瘤细胞系。 WHO II K1861-10系不完全抑制(最大抑制69%),Triciribine的GI50值为1.7μM。 Triciribine在1-10μM时表现出最大的生长抑制,并抑制Akt磷酸化以及下游p70S6K在KR158细胞中达到100μM(IC50 = 130 nM)的基础水平[2]。 Triciribine(TCN)是一种具有已知抗肿瘤活性的新型三环类化合物。使用合胞体斑块测定,Triciribine对0.01-0.02μM的HIV-1具有活性。使用微量滴定XTT试验,Triciribine对一组HIV-1和HIV-2菌株具有活性,IC50值范围为0.02至0.46μM[3]。 |
In Vivo | Triciribine(TCBN)治疗,在缺氧14天至缺氧21天后给药7天,逆转血管增厚,如免疫组织化学和Western分析所示。另一方面,雷帕霉素治疗不能预防缺氧引起的肺泡出血和充血。 Triciribine部分抑制了脉管系统的进行性修剪,这支持了我们之前的发现,即Triciribine缓解了微毛细血管的血管闭塞。相比之下,雷帕霉素治疗并未显著逆转由于慢性缺氧引起的血管密度降低,并且对小血管的修剪没有显著影响[4]。 |
Cell Experiment | 将人SF295和U87MG GBM系和小鼠K1861-10,KR158和KR130G星形细胞瘤系以2500个细胞/100μL完全培养基的密度接种在96孔板中。将小鼠原代星形胶质细胞以5000个细胞/100μL铺板。用连续稀释的抑制剂(测试的抑制剂是PI-103,Triciribine和雷帕霉素)处理细胞一式三份,范围从μM到pM。在Novostar平板读数器上使用Alamar Blue测定法在3天后测量细胞增殖。使用GraphPad Prism v4和Microsoft Excel [2]中的标准程序计算50%抑制浓度(IC 50)和50%生长抑制浓度(GI 50)的值。 |
Animal Experiment | 对小鼠[4] Akt1 +/+和Akt1 - / - 小鼠进行常氧或缺氧(10%O2)7天和14天(每组n = 2-6只小鼠)。值得注意的是,在暴露于缺氧超过14-16天的Akt1 - / - 小鼠中观察到高死亡率。对于药理学抑制研究,接受常氧或慢性缺氧14天的Akt1 +/+小鼠每天腹腔注射生理盐水,Triciribine(0.5 mg/kg /天)或雷帕霉素(1.5 mg/kg /天),持续7天,并且持续暴露于缺氧或常氧是21天(每组n = 6-8只小鼠)。每天施用药理学抑制剂,同时将小鼠维持在缺氧室中以最小化暴露于空气和肺重塑的自发逆转。 |
Data Literature Source | [1]. Dieterle A,et al. The Akt inhibitor triciribine sensitizes prostate carcinoma cells to TRAIL-induced apoptosis. Int J Cancer. 2009 Aug 15;125(4):932-41. [2]. Gürsel DB,et al. Control of proliferation in astrocytoma cells by the receptor tyrosine kinase/PI3K/AKT signaling axis and the use of PI-103 and TCN as potential anti-astrocytoma therapies. Neuro Oncol. 2011 Jun;13(6):610-21. [3]. Kucera LS,et al. Activity of triciribine and triciribine-5'-monophosphate against human immunodeficiency virus types 1 and 2. AIDS Res Hum Retroviruses. 1993 Apr;9(4):307-14. [4]. Abdalla M,et al. The Akt inhibitor,triciribine,ameliorates chronic hypoxia-induced vascular pruning and TGFβ-induced pulmonary fibrosis. Br J Pharmacol. 2015 Aug;172(16):4173-88. |
Unit | Bottle |
Specification | 5mg |
Triciribine 是一种 DNA 合成 (DNA synthesis) 抑制剂,也抑制 Akt 和 HIV-1/2。