Triciribine (API-2)
别名: NSC 154020, VD-0002, vqd-002, TCN 中文名称：曲西立滨
Triciribine (API-2)是一种DNA synthesis抑制剂，也抑制PC3细胞系中的Akt和CEM-SS，H9，H9IIIB，U1细胞中的HIV-1，IC50分别为130 nM和20 nM；对PI3K/PDK1没有抑制作用；作用于缺乏腺苷激酶的细胞，活性降低5000倍。Phase 1/2。
Triciribine (API-2) Chemical Structure
CAS: 35943-35-2
客户使用Selleck的Triciribine (API-2)发表文献90篇
产品质控
批次：
纯度：
99.70%
99.70
Triciribine (API-2)相关产品
| 相关靶点 | Akt1 Akt2 Akt3 | 点击展开 |
|---|---|---|
| 相关化合物库 | 激酶抑制剂库 PI3K/Akt 抑制剂库 凋亡分子化合物库 细胞周期化合物库 NF-κB信号通路库 | 点击展开 |
相关信号通路图
Akt抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 184B5 | Cytotoxicity assay | 20 uM | Cytotoxicity against human 184B5 cells at 20 uM chloroquine by SRB assay, GI50=16.96μM | 18691894 | |
| MDA-MB-468 | Cytotoxicity assay | 10 uM | Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay, GI50=20.45μM | 18691894 | |
| 184B5 | Cytotoxicity assay | 10 uM | Cytotoxicity against human 184B5 cells at 10 uM chloroquine by SRB assay, GI50=34μM | 18691894 | |
| MDA-MB-231 | Cytotoxicity assay | 10 uM | Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay, GI50=37μM | 18691894 | |
| AA2 | Function assay | 5 hrs | Intracellular phosphorylation (100 uM) in uninfected AA2 cells was studied after 5 hrs of Incubation., Concentration=9μM | 10882373 | |
| MDM | Antiviral assay | 6 days | Antiviral activity against Human immunodeficiency virus 1 ADA infected in human MDM cells assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50=0.006μM | 20086149 | |
| CEM-SS | Antiviral assay | 6 days | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 0.78 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50<0.01μM | 20086149 | |
| MDM | Antiviral assay | 6 days | Antiviral activity against Human immunodeficiency virus 1 BAL infected in human MDM cells assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50=0.018μM | 20086149 | |
| H9 | Antiviral assay | 6 days | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 12.5 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50<0.1μM | 20086149 | |
| H9 | Antiviral assay | 6 days | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 6.25 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50<0.1μM | 20086149 | |
| ACH2 | Antiviral assay | 3 days | Antiviral activity against 5 x 10'3 cells/well Human immunodeficiency virus 1 infected in human ACH2 cells assessed as inhibition of viral Reverse transcriptase after 3 days by [3H]TTP incorporation assay in presence of 5 ng/ml tumor necrosis factor alpha, IC50=0.15μM | 20086149 | |
| CEM-SS | Antiviral assay | 6 days | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 1.56 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50=0.19μM | 20086149 | |
| CEM-SS | Antiviral assay | 6 days | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 3.13 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA, IC50=0.24μM | 20086149 | |
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay, GI50=0.56μM | 18691894 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells in presence of 20 uM chloroquine by SRB assay, GI50=0.05μM | 18691894 | ||
| Huh-7 | Function assay | Compound was tested for its ability to inhibit hepatitis C viral RNA replication in Huh-7 cells (human hepatoma cells), EC50=2μM | 15177464 | ||
| BSC-1 | Antiviral assay | Antiviral activity against HSV-1 was determined using BSC-1 cells by an enzyme-linked immunosorbent assay (ELISA), IC50=23μM | 10882373 | ||
| HFF | Antiviral assay | Antiviral activity against HCMV was determined by plaque reduction assay using HFF cells, IC50=2.5μM | 10882373 | ||
| BSC-1 | Antiviral assay | Antiviral activity was tested using an enzyme-linked immunosorbent assay (ELISA) to detect HSV-1 (herpes simplex virus type 1) using BSC-1 cells, IC50=23μM | 10882371 | ||
| HFF | Function assay | HCMV plaque assay was performed using HFF cells and effect was calculated as a percentage of reduction in number of plaques, IC50=2.5μM | 10882371 | ||
| L1210 | Function assay | Tested in vitro for cytotoxicity against murine L1210 leukemic cells, IC50=0.035μM | 10882371 | ||
| MDA-MB-231 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-231 cells in presence of 20 uM chloroquine by SRB assay, GI50=0.69μM | 18691894 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells by SRB assay, GI50=3.64μM | 18691894 | ||
| MDA-MB-468 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay, GI50=10.29μM | 18691894 | ||
| 184B5 | Cytotoxicity assay | Cytotoxicity against human 184B5 cells by SRB assay, GI50=40μM | 18691894 | ||
| MDA-MB-468 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-468 cells by SRB assay, GI50=43.53μM | 18691894 | ||
| ACH2 | Cytotoxicity assay | Cytotoxicity against human ACH2 cells infected with latent Human immunodeficiency virus 1 by MTS assay, CC50=0.01μM | 20086149 | ||
| ACH2 | Cytotoxicity assay | Cytotoxicity against human ACH2 cells infected with latent Human immunodeficiency virus 1 by MTS assay in presence of tumor necrosis factor alpha, CC50=0.01μM | 20086149 | ||
| H9 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 SK1 infected in human H9 cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.036μM | 20086149 | ||
| CEM-SS | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B expressing nef protein infecting in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.04μM | 20086149 | ||
| CEM-SS | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 0.78 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.08μM | 20086149 | ||
| H9 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 25 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.1μM | 20086149 | ||
| H9 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 12.5 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.1μM | 20086149 | ||
| H9 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 6.25 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.1μM | 20086149 | ||
| CEM-SS | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 SK1 infected in human CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.13μM | 20086149 | ||
| AA5 | Antiviral assay | Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 3.13 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.17μM | 20086149 | ||
| AA5 | Antiviral assay | Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 1.56 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.17μM | 20086149 | ||
| AA5 | Antiviral assay | Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 0.78 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50<0.17μM | 20086149 | ||
| CEM-SS | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 harboring plasmid NL4-3 infected in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.2μM | 20086149 | ||
| U1 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 infected in human U1 cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.23μM | 20086149 | ||
| U1 | Cytotoxicity assay | Cytotoxicity against human U1 cells infected with latent Human immunodeficiency virus 1 by MTS assay, CC50=0.28μM | 20086149 | ||
| U1 | Cytotoxicity assay | Cytotoxicity against human U1 cells infected with latent Human immunodeficiency virus 1 by MTS assay in presence of tumor necrosis factor alpha, CC50=0.28μM | 20086149 | ||
| CEM-SS | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 1.56 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.29μM | 20086149 | ||
| CEM-SS | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 3.13 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.3μM | 20086149 | ||
| CEM-SS | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 D1 harboring Tyr127His mutation in nef protein infecting in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.33μM | 20086149 | ||
| CEM-SS | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 A7 harboring Tyr127His mutation in nef protein infecting in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=0.5μM | 20086149 | ||
| MDM | Cytotoxicity assay | Cytotoxicity against human MDM cells infected with Human immunodeficiency virus 1 BAL by MTS assay, TC50=0.66μM | 20086149 | ||
| CEM-SS | Antiviral assay | Antiviral activity against Human immunodeficiency virus 2 ROD infected in human CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=1.4μM | 20086149 | ||
| H9 | Antiviral assay | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 50 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay, IC50=1.53μM | 20086149 | ||
| H9 | Cytotoxicity assay | Cytotoxicity against human H9 cells by MTS assay, IC50=16.3μM | 20086149 | ||
| H9 | Cytotoxicity assay | Cytotoxicity against human H9 cells by MTS assay, CC50=19.6μM | 20086149 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Triciribine (API-2)是一种DNA synthesis抑制剂，也抑制PC3细胞系中的Akt和CEM-SS，H9，H9IIIB，U1细胞中的HIV-1，IC50分别为130 nM和20 nM；对PI3K/PDK1没有抑制作用；作用于缺乏腺苷激酶的细胞，活性降低5000倍。Phase 1/2。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Triciribine的剂量为1-10 μM时生长抑制的效果最佳。像dosnstream p70S6K一样Triciribine基本在100μM (IC50 = 130 nM)时可以抑制Akt的磷酸化作用。Triciribine抑制Nf1和Trp53突变的肿瘤星型细胞的生长，这种抑制具有梯度依赖的特性。Triciribine在GI50为1.7 μM时并不能完全抑制（最高可抑制率为69%）WHO II K1861-10系的生长，而对于更高级的肿瘤系(KR158, KR130, and SF295), Triciribine可以在更低的GI50值(0.4–1.1 mM)时产生更广泛的抑制（最高抑制率>80%）。重要的是Triciribine能特异性地抑制肿瘤细胞而对大多数普通的星形胶质细胞抑制效率很低(GI50¼13.6 mM) [1]。Triciribine能抑制HIV-1， IC50为20 nM。用量为0.1μM时能产生>90%的抑制率，用量为5μM时能完全抑制多核体的形成。 在相同的细胞系中相关的细胞毒性实验结果显示当 Triciribine 浓度为46 μM时的选择性指数为2250. 利用HIV-1急性感染的CEM-SS, h9, 和 持续感染的H9III B 和 U1 细胞研究发现， Triciribine 可以显著的抑制HIV-1诱导的 p24 核心抗原的产生, 反转录酶和传染性病毒的产生，这种抑制具有剂量依赖的特性[2]。 Triciribine会抑制人前列腺癌PC-3 细胞系中的Akt 308位的酸酸和473位丝氨酸的磷酸化 以及Akt 的活性. Triciribine使PC-3 细胞对于TRAIL- 和 anti-CD95诱导的细胞凋亡更加敏感, 但是对于能引起DNA损伤的化疗依然具有抗性[3]。Triciribine 对于Akt具有高度的选择性，并不会抑制其它激酶的激活，如磷脂酰肌醇3激酶, 磷酸肌醇依赖的激酶1, 蛋白激酶C, serumand 糖皮质激素诱导激酶, 蛋白激酶 A, 信号传感器 和转录3 活化剂, 胞外信号调节激酶1/2或者c-Jun NH2-末端 激酶[4]。 | |||
|---|---|---|---|---|
| 激酶实验 | Akt磷酸化改变分析 | |||
| 待细胞生长到全板80%–90%，加入1–10 ng/mL表皮生长因子(EGF; cat #01-107)或血小板生长因子(PDGF)–AA (cat #01-309) (Upstate Biotechnology)加入或者不加 10–20 mM的 U0126 (cat #EI-282) 或 LY-294002 (cat #ST-420) (Biomol Research Lab)刺激细胞5到10分钟。用12%–15% SDS PAGE分离5–20 μg蛋白裂解液，用Akt (cat #cs-9272), 磷酸化的 Akt (磷酸丝氨酸 473; cat #cs-9271), MAPK (cat #cs-9102)和磷酸化 MAPK (p44/42 磷酸苏氨酸202/Tyr204; cat #cs-01-9101)抗体1:1000稀释（Cell Signaling Technology)蛋白印迹检测蛋白裂解物。 | ||||
| 细胞实验 | 细胞系 | CEM-SS 细胞 | ||
| 浓度 | 0-500 μM | |||
| 孵育时间 | 48小时 | |||
| 方法 | 将 CEM-SS细胞按1万个每孔的密度接种在96孔平板中并在生长培养基中培养，用上述细胞对triciribine的细胞毒性进行分析评定. 将连续稀释5倍的不同浓度的Triciribine加到细胞中. 37℃孵育48小时, 通过电转将细胞用含有放射性同位素3H的 dThd (1 μCi 每孔, 放射性比度为20 Ci/mmol)标记6小时，收取细胞并测定总的DNA合成量 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | PUMA / p-FoxO3a / p-AKT |
|
20978166 | |
| Immunofluorescence | TRF2 / 53BP1 |
|
23862686 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Riciribine按照 1 mg/kg/天的剂量对裸小鼠腹腔注射，可以抑制 OVCAR3, OVCAR8 和 PANC1 肿瘤的生长, 分别使Akt过量表达了90%, 88% 和80%。 然而, Triciribine 对OVCAR5 和 COLO357细胞的生长基本没有影响[4]。 | |
|---|---|---|
| 动物实验 | Animal Models | 皮下注射OVCAR3, OVCAR8, PANC1, OVCAR5和 COLO357 肿瘤细胞的80周龄雌性裸小鼠. |
| Dosages | 1 mg/kg/天 | |
| Administration | 腹腔注射，一天一次. | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02987127 | Unknown status | Mucosa-Associated Lymphoid Tissue Lymphoma |
National Taiwan University Hospital |
February 2016 | -- |
| NCT00642031 | Completed | Hematologic Malignancies|Leukemia |
Prescient Therapeutics Ltd.|VioQuest Pharmaceuticals |
August 2006 | Phase 1 |
化学信息&溶解度
| 分子量 | 320.3 | 分子式 | C13H16N6O4 |
| CAS号 | 35943-35-2 | SDF | Download Triciribine (API-2) SDF |
| Smiles | CN1C2=NC=NC3=C2C(=CN3C4C(C(C(O4)CO)O)O)C(=N1)N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 64 mg/mL ( (199.81 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 16 mg/mL Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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