产品说明书

Triciribine

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Chemical Structure| 35943-35-2 同义名 : API-2;TCN;Tricyclic Nucleoside;vqd-002;VD-0002;NSC 154020
CAS号 : 35943-35-2
货号 : A930307
分子式 : C13H16N6O4
纯度 : 99%+
分子量 : 320.304
MDL号 : MFCD00932413
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(327.81 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Akt

    Akt, IC50:130 nM
描述 Triciribine (TCN) is a purine analog which is initially shown to inhibit DNA synthesis. Triciribine selectively inhibits the phosphorylation and activation of all three Akt isoforms. At a concentration of 10 μM Triciribine Akt phosphorylation is inhibited at both Thr308 and Ser473. Triciribine effectively inhibits the phosphorylation and consequently the catalytic activity of Akt in PC-3 cells[1]. While Triciribine does not efficiently inhibit the U87MG human cell line, it shows selective inhibition against other astrocytoma cell lines based on their grade. The WHO II K1861-10 line shows a partial response (69% maximum inhibition) with a GI50 of 1.7 μM. Optimal growth suppression by Triciribine occurs between 1-10 μM, reducing Akt phosphorylation and the activity of downstream p70S6K to baseline levels at 100 μM (IC50=130 nM) in KR158 cells[2]. Triciribine, a novel tricyclic compound with antitumor properties, demonstrates effectiveness against HIV-1 in a syncytial plaque assay at concentrations of 0.01-0.02 μM. Additionally, it is active against various strains of HIV-1 and HIV-2, with IC50 values ranging from 0.02 to 0.46 μM in a microtiter XTT assay[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
AA5 cells Function 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=0.17 μM 20086149
HFF cells Function assay HCMV plaque assay was performed using HFF cells and effect was calculated as a percentage of reduction in number of plaques, IC50=2.5 μM 10882371
Huh-7 cells Function assay Compound was tested for its ability to inhibit hepatitis C viral RNA replication in Huh-7 cells (human hepatoma cells), EC50=2 μM 15177464
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02515773 Bipolar Disorder Phase 4 Recruiting October 2020 United States, Kentucky ... 展开 >> The Children's Home of Northern Kentucky Recruiting Covington, Kentucky, United States, 41011 Contact: Joe Reiman    859-292-4122    jrieman@chnk.org    United States, New Jersey Jersey Shore Medical Center Not yet recruiting Neptune City, New Jersey, United States, 07753 Contact: Nicholas Remo    732-776-3498    NRemo@meridianhealth.com    United States, New York South Oaks Recruiting Amityville, New York, United States, 11701 Contact: Patricia Flaherty, LCSW-R,ACSW,    631-608-5222    pflaherty@northwell.edu    SUNY Downstate/ Kings County Hospital Not yet recruiting Brooklyn, New York, United States, 11203 Contact: Cathryn A. Galanter, M.D.    718-245-2502    cathryn.galanter@downstate.edu    Maimonides Not yet recruiting Brooklyn, New York, United States, 11219 Contact: George Alvarado, M.D.    718-283-8215    GAlvarado@maimonidesmed.org    NYCCC Not yet recruiting Brooklyn, New York, United States, 11233 Contact: Eva Sheridan    718-470-4391    eschenk@northwell.edu    Northwell Zucker Long Island Jewish Hospital Recruiting Glen Oaks, New York, United States, 11004 Contact: Arielle Carmel    718-470-8021    acarmel@northwell.edu    Mount Sinai Recruiting New York, New York, United States, 10029 Contact: Julia G Jones    212-241-3692    julia.george-jones@mssm.edu    LIJ Zucker Hillside Hospital Recruiting New York, New York, United States, 11004 Contact: Eva Shenck    718-470-4391    eschenk@northwell.edu    Child Center of New York, Recruiting Queens, New York, United States, 11373 Contact: Isaiah Mui    718-358-8288 ext 221    isaiahmui@childcenterny.org    Contact: Alla Weinstein    718.358.8288    allaweinstein@childcenterny.org    NorthShore Child and Family Guidance Recruiting Roslyn Heights, New York, United States, 11577 Contact: Esther Gonzalez    516-626-1971    EGonzalez@northshorechildguidance.org    StonyBrook Recruiting Stony Brook, New York, United States, 11794 Contact: Gabrielle A Carlson, MD    631-632-8840    Gabrielle.Carlson@stonybrookmedicine.edu    United States, Ohio Lighthouse Youth Services Recruiting Cincinnati, Ohio, United States, 45206 Contact: Jody Harding    513-487-6778    jarding@lys.org    Contact: Shannon Kiniyalocts    513-487-7706    skiniyalocts@lys.org    Central Clinic Recruiting Cincinnati, Ohio, United States, 45219 Contact: Maria Piombo, Ed.D.,LPCC-S    513-558-5890    piombom@ucmail.uc.edu    Children's Home Recruiting Cincinnati, Ohio, United States, 45227 Contact: Jessica Aritonovich    513-272-2800 ext 4352    jaritonovich@thechildrenshomecinti.org    Cincinnati Children's Hospital Medical Center Recruiting Cincinnati, Ohio, United States, 45229 Contact: Elizabeth Picard, MS    513-803-8898    elizabeth.picard@cchmc.org    Contact: Shelley Randall    513-803-2342    Shelley.randall@cchmc.org    Resident Mood Medication Clinic Recruiting Cincinnati, Ohio, United States, 45229 Contact: Christy Klein, MPH    513-558-5746    kleinci@ucmail.uc.edu    St. Aloysius Recruiting Cincinnati, Ohio, United States, 45237 Contact: Morrisa Gray, RN, BSN    513-482-7257    mgray@stalsorphanage.org    Talbert House Recruiting Cincinnati, Ohio, United States, 45238 Contact: Sharon Stanford, MD    513-265-6090    sharon.stanford@talberthouse.com    St. Joseph's Orphanage Recruiting Cincinnati, Ohio, United States, 45239 Contact: Tyann Godwin, RN    513-741-3100 ext 2166    tyann.godwin@sjokids.org    Child Focus Recruiting Cincinnati, Ohio, United States, 45244 Contact: Jessica Bowlin       JBowlin@child-focus.org    NECCO Recruiting Cincinnati, Ohio, United States, 45246 Contact: Jessica Parks, MSM, LISW-S    513-771-9600    jparks@necco.org    University Hospital Medical Center Cleveland Recruiting Cleveland, Ohio, United States, 44106 Contact: Elizabeth Deyling       Elizabeth.Deyling@UHhospitals.org    Nationwide Children's Hospital Columbus Recruiting Columbus, Ohio, United States, 43205 Contact: Raymond Troy       raymond.troy@nationwidechildrens.org    Ohio State University Recruiting Columbus, Ohio, United States, 43210 Contact: Ghada Lteif, MD    614-293-8237    ghada.lteif@osumc.edu    South Community Recruiting Dayton, Ohio, United States Contact: Mary Day, RN    937-245-6121    mday@southcommunity.com    Butler Behavioral Health Services Recruiting Hamilton, Ohio, United States, 45011 Contact: Randy Allman, LISW-S    513-881-7189 ext 3134    Rallman@bbhs.org    TCN Family Solutions Recruiting Xenia, Ohio, United States, 45385 Contact: Carmel Flores    937-427-3837    cflores@tcn.org    United States, Texas Seton Family of Hospitals Not yet recruiting Austin, Texas, United States, 78712 Contact: Ashleigh Smith       AJSmith2@seton.org 收起 <<
NCT01098812 Cataract Phase 3 Completed - United States, California ... 展开 >> AMO Clinical Research Call Center for Trial Locations Santa Ana, California, United States, 92705 收起 <<
NCT02332005 Diabetic Peripheral Neuropathy Phase 2 Phase 3 Completed - Russian Federation ... 展开 >> City Hospital No 40 of the Kurortny District St Petersburg, Sestroretsk, Russian Federation, 197706 Northern State Medical University Arkhangelsk, Russian Federation, 163000 Health Services Severstal Cherepovets, Russian Federation, 162600 Clinic of Neurology Ekaterinburg, Russian Federation, 620014 Kemerovo Regional Clinical Hospital Kemerovo, Russian Federation, 650066 Endocrinology Dispensary Moscow, Russian Federation, 119034 Morozovskaya Children City Hospital of Moscow Moscow, Russian Federation, 119049 I M Sechenov First Moscow State Medical University Moscow, Russian Federation, 119435 IM Sechenov First Moscow State Medical University Moscow, Russian Federation, 119435 IM Sechenov First Moscow State Medical University Moscow, Russian Federation, 119991 City Clinical Hospital No 71 Moscow, Russian Federation, 121374 Central Clinical Hospital No 1 of JSC Russian Railway Moscow, Russian Federation, 125367 City Clinical Hospital No 50 Moscow, Russian Federation, 127206 The Federal Bureau of Medical and Social Expertise Moscow, Russian Federation, 127486 Perm State Medical Academy Perm, Russian Federation, 614107 VA Baranov Respublical Hospital Petrozavodsk, Russian Federation, 185019 Rostov State Medical University Rostov-on-Don, Russian Federation, 344022 City Polyclinic No 20 Saratov, Russian Federation, 410053 Imc Sogaz St Petersburg, Russian Federation, 191186 Medical Center Reavita St Petersburg, Russian Federation, 194295 City Hospital of the Holy Martyr Elizabeth St Petersburg, Russian Federation, 195257 Nikolaev Hospital St Petersburg, Russian Federation, 198510 Bashkir State Medical University Ufa, Russian Federation, 450000 Central City Clinical Hospital Ulyanovsk, Russian Federation, 432057 State Medical University Volgograd, Russian Federation, 400131 Regional Clinical Hospital Yaroslavl, Russian Federation, 150000 NV Solovyov Clinical Emergency Hospital Yaroslavl, Russian Federation, 150003 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.61mL

3.12mL

1.56mL

31.22mL

6.24mL

3.12mL
参考文献

[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. 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.