Triciribine

产品编号 T6065   CAS 35943-35-2
别名: NSC 154020, TCN, API-2, VD-0002, Tricyclic nucleoside, VD-0002, Tricyclic nucleoside, TCN, NSC 154020 API-2

Triciribine is a DNA synthesis inhibitor, and it also inhibits Akt and HIV-1/2.

Triciribine结构式
Triciribine , CAS 35943-35-2
规格 库存 价格/RMB 数量
2 mg 上海现货 420.00
5 mg 上海现货 810.00
10 mg 上海现货 1120.00
25 mg 上海现货 2260.00
50 mg 上海现货 3880.00
100 mg 上海现货 6984.00
1 mL * 10 mM (in DMSO) 上海现货 810.00
大包装特惠,请咨询
选择批次  
纯度 99.87%
纯度 100.00%
生物活性
化学信息
存储 & 溶解度
Preparing Solutions
产品描述 Triciribine is a DNA synthesis inhibitor, and it also inhibits Akt and HIV-1/2.
靶点活性 Akt : ic50 130nM ,   HIV-1 : ic50 20nM
体外活性 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). Triciribine 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 Triciribine, 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, Triciribine is much less effective at inhibiting primary astrocytes (GI5013.6 mM), suggesting that this inhibitor may show specificity for tumor cells. [1] Triciribine inihibits HIV-1with an IC50 of 20 nM. Greater than 90% inhibition is achieved at 0.1 μM and complete inhibition of syncytia formation is achieved at 5 μM. Associated cell toxicity in the same cell line for Triciribine is 46 μM, resulting in selectivity indices of 2250. Triciribine 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. [2] Triciribine inhibits Akt phosphorylation at Thr308 and Ser473 and Akt activity in the human prostate cancer cell line PC-3. Triciribine sensitizes PC-3 cells to TRAIL- and anti-CD95-induced apoptosis, whereas the cells remain resistant to DNA damaging chemotherapeutics. [3] Triciribine 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. [4]
体内活性 1 mg/kg/day i.p. treated Triciribine inhibits OVCAR3, OVCAR8 and PANC1 tumor growth, which overexpressing Akt, by 90%, 88% and 80% in nude mice, respectively. However, Triciribine has little effect on the growth of OVCAR5 and COLO357 cells. [4]
Kinase Assay Akt Phosphorylation Changes Assay: 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).
Cell Research
Triciribine 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 Triciribine 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.(Only for Reference)
Cell lines: CEM-SS cells
Animal Research
Animal Model: OVCAR3, OVCAR8, PANC1, OVCAR5 and COLO357 tumor cells are injected s.c. into 80week-old fenude mice.
别名 NSC 154020 , TCN , API-2 , VD-0002 , Tricyclic nucleoside , VD-0002 , Tricyclic nucleoside , TCN , NSC 154020 API-2
纯度 100.00%
分子量 320.3
分子式 C13H16N6O4
CAS No. 35943-35-2

存储

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

溶解度

1eq. HCl: 32 mg/mL (100 mM)

DMSO: 32 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

1% DMSO/30% polyethylene glycol/1% Tween 80: 30 mg/mL

文献引用

参考文献
1. Gursel DB, et al, Nero Oncol, 2011, 13(6), 610-621. 2. Kucera LS, et al, AIDS Res Hum Retroviruses, 1993, 9(4), 307-314. 3. Dieterle A, et al, Int J Cancer , 2009, 125(4), 932-941. 4. Yang L, et al, Cancer Res, 2004, 64(13), 4394-4399. 5. 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.

Related Compound Libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Anti-infection Compound Library PI3K-AKT-mTOR Compound Library Protease Inhibitor Library Anti-virus Compound Library DNA Damage & Repair Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library

相关产品

具有相同靶点的化合物
Karanjin RN-18 A-674563 2HCl(552325-73-2(fb-2hcl)) Triciribine AT7867 Liquidambaric lactone Ilexgenin A Cytochalasin D

剂量换算

对于各种应用,安全且有效的用药剂量是很有必要的 了解更多

体内实验配液计算器

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
ul
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

计算器

摩尔计算器
稀释计算器
配液计算器
分子量计算器
=
X
X

Molarity Calculator allows you to calculate the

  • mass of a compound required to prepare a solution of known volume and concentration
  • volume of solution required to dissolve a compound of known mass to a desired concentration
  • concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

技术支持

Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.

 

陶素的所有产品和服务仅用于科学研究,我们不为任何其他用途提供产品和服务,也不为任何个人提供产品和服务。
微信公众号
Copyright © 2018 Topscience Co. Ltd. All rights reserved. 沪ICP备20019793号-2 沪公网安备 31010602004043号