Structure of Triciribine
CAS No.: 35943-35-2
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Triciribine serves as a DNA synthesis inhibitor and also inhibits Akt and HIV-1/2 with IC50 values of 130 nM and 0.02-0.46 μM, respectively.
Synonyms: API-2; TCN; Tricyclic Nucleoside
4.5
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| CAS No. : | 35943-35-2 |
| Formula : | C13H16N6O4 |
| M.W : | 320.30 |
| SMILES Code : | NC1=NN(C)C2=NC=NC3=C2C1=CN3[C@H]4[C@@H]([C@@H]([C@@H](CO)O4)O)O |
| Synonyms : |
API-2; TCN; Tricyclic Nucleoside
|
| MDL No. : | MFCD00932413 |
| InChI Key : | HOGVTUZUJGHKPL-HTVVRFAVSA-N |
| Pubchem ID : | 65399 |
| GHS Pictogram: |
|
| Signal Word: | Warning |
| Hazard Statements: | H317-H319 |
| Precautionary Statements: | P280-P305+P351+P338 |
| Target |
|
In Vitro:
|
Cell Line
|
Concentration | Treated Time | Description | References |
| SUM159 cells | 20 μM | 3 h | Inhibition of Akt activity, reduction of Runx2 target gene expression | J Cell Physiol. 2013 Aug;228(8):1784-92. |
| Caco2 cells | 1 μM | 60 min | To study the effect of Triciribine on Ang II-induced inhibition of Pgp activity, results showed that Triciribine blocked the inhibitory effect of Ang II on Pgp activity. | Acta Physiol (Oxf). 2020 Jan;228(1):e13332. |
| Mouse cardiac fibroblasts (MCF) | 1 µM or 10 µM | 6 days | Triciribine was able to abolish the effect of circ-Amotl1 on promoting MCF cell proliferation. | Theranostics. 2017 Aug 29;7(16):3842-3855. |
| Mouse cardiac fibroblasts (MCF) | 1 µM | 3 days | 1 µM Triciribine was able to abolish the effect of circ-Amotl1 on promoting MCF cell proliferation after 3 days. | Theranostics. 2017 Aug 29;7(16):3842-3855. |
| Mouse cardiac fibroblasts (MCF) | 0.1 µM | 3 days | 0.1 µM Triciribine was able to abolish the effect of circ-Amotl1 on repressing MCF cell apoptosis after 3 days. | Theranostics. 2017 Aug 29;7(16):3842-3855. |
| Adipoq−/− VSMCs | 10 µM | 24 h | Inhibition of AKT and MAPK1 signaling pathways, reducing cell proliferation and migration, and partially restoring the contractile phenotype of VSMCs. | Cells. 2023 Oct 20;12(20):2493. |
| Caco2 cells | 1 μM | 1 h | Triciribine blocked the inhibitory effects of Ang II on Pgp function, indicating that Akt plays a key role in Ang II-mediated inhibition of Pgp function. | Acta Physiol (Oxf). 2020 Jan;228(1):e13332. |
| HNSCC cells | 5 μM | 24 h | Inhibition of AKT activation, significantly suppressed BDNF-mediated cellular motility | Oncogene. 2010 Apr 8;29(14):2047-59. |
In Vivo:
|
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
| Mice | APAP-induced liver injury model | Intraperitoneal injection | 1 mg/kg | Single dose, ALT measured at 24 hours post-APAP | Inhibition of Akt signaling aggravated APAP-induced liver injury | Hepatology. 2017 Nov;66(5):1601-1615 |
| Mice | ARHGEF3-KO mice | Intraperitoneal injection | 1 mg/kg | Every 24 hours until the end of the experiment | Triciribine inhibited the phosphorylation of Akt but did not prevent the enhanced muscle regeneration and strength recovery in ARHGEF3-KO mice, indicating that the promotion of muscle regeneration by ARHGEF3 knockout is independent of the Akt signaling pathway. | Cell Rep. 2021 Jan 5;34(1):108594 |
Clinical Trial:
| NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
| NCT02515773 | Bipolar Disorder | Phase 4 | Recruiting | October 2020 | United States, Kentucky ... More >> 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 Less << |
| NCT01098812 | Cataract | Phase 3 | Completed | - | United States, California ... More >> AMO Clinical Research Call Center for Trial Locations Santa Ana, California, United States, 92705 Less << |
| NCT02332005 | Diabetic Peripheral Neuropathy | Phase 2 Phase 3 | Completed | - | Russian Federation ... More >> 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 Less << |
| NCT03326713 | Breast Cancer ... More >> Ovarian Cancer Less << | Not Applicable | Recruiting | September 1, 2021 | United States, New Mexico ... More >> University of New Mexico Recruiting Albuquerque, New Mexico, United States, 87131 Contact: Anita Y Kinney, PhD, RN 505-925-0731 AYKinney@salud.unm.edu Less << |
| NCT01863290 | - | Completed | - | United States, Alabama ... More >> University of Alabama Birmingham, Alabama, United States, 25294-4410 United States, California Contra Costa Health Services (East and West Contra Costa) Martinez, California, United States, 94553 Southeast Health Center San Francisco, California, United States, 94103 Santa Clara Health Center San Jose, California, United States, 95128 United States, Connecticut Yale Primary Care Center New Haven, Connecticut, United States, 06520 United States, Maryland East Baltimore Medical Center Baltimore, Maryland, United States, 21287 United States, Massachusetts Boston Healthcare for the Homeless Program Boston, Massachusetts, United States, 02118 United States, New York Morningside Clinic New York, New York, United States, 10025 Montefiore Transition Clinic New York, New York, United States, 10467 Medicine in Psychiatry Service clinic of the University of Rochester Medical Center Rochester, New York, United States, 14642 Puerto Rico Corporacion SANOS Caguas, Puerto Rico, 00725 Less << | |
| NCT02860013 | Heart Failure | Not Applicable | Unknown | - | - |
| NCT00747565 | Cataract | Not Applicable | Completed | - | - |
| NCT01098812 | - | Completed | - | - | |
| NCT01594437 | Cytomegalovirus Infections | Phase 1 | Completed | - | United States, Maryland ... More >> SNBL Clinical Pharmacology Center Baltimore, Maryland, United States, 21201 Less << |
| NCT00747565 | - | Completed | - | - | |
| NCT01697293 | Breast Adenocarcinoma ... More >> Estrogen Receptor Positive HER2/Neu Negative Recurrent Breast Carcinoma Stage IIB Breast Cancer Stage IIIA Breast Cancer Stage IIIB Breast Cancer Stage IIIC Breast Cancer Stage IV Breast Cancer Less << | Phase 1 Phase 2 | Recruiting | January 2019 | United States, Florida ... More >> Moffitt Cancer Center Recruiting Tampa, Florida, United States, 33612 Contact: Hyo S. Han 813-745-8480 hyo.han@moffitt.org Principal Investigator: Hyo S. Han United States, New York Albert Einstein College of Medicine Recruiting Bronx, New York, United States, 10461 Contact: Joseph A. Sparano 718-405-8404 jsparano@montefiore.org Principal Investigator: Joseph A. Sparano Less << |
| NCT01984840 | Pulmonary Disease, Chronic Obs... More >>tructive Less << | Not Applicable | Completed | - | Denmark ... More >> Aalborg University Aalborg, Denmark, 9220 Less << |
| NCT02930109 | Acute Leukemia | Phase 1 Phase 2 | Recruiting | December 2018 | United States, Connecticut ... More >> Yale Cancer Center Recruiting New Haven, Connecticut, United States, 06520-8028 Contact: Anne Caldewell 475-434-7321 anne.caldwell@yale.edu Contact: Rebecca Lilian rebecca.lilian@yale.edu Principal Investigator: Thomas Prebet, MD United States, Florida Moffitt Cancer Center Recruiting Tampa, Florida, United States, 33612 Contact: Nancy Hillgruber nancy.hillgruber@moffitt.org Principal Investigator: Jeffrey Lancet, MD Less << |
| NCT01390025 | Influenza, Human | Phase 1 | Completed | - | United States, Maryland ... More >> SNBL Clinical Pharmacology Center Baltimore, Maryland, United States, 21201 Less << |
| NCT01719874 | Influenza | Phase 2 | Unknown | March 2013 | United Kingdom ... More >> Recruiting London, United Kingdom Less << |
| NCT01690468 | Ovarian Cancer | Phase 1 Phase 2 | Recruiting | December 2018 | United States, Florida ... More >> H. Lee Moffitt Cancer Center and Research Institute Recruiting Tampa, Florida, United States, 33612 Contact: Denise Dorman 813-745-7272 denise.dorman@moffitt.org Sub-Investigator: Sachin Apte, M.D. Principal Investigator: Robert M. Wenham, M.D. Sub-Investigator: Mian Shahzad, M.D., Ph.D. Less << |
| NCT00363454 | Cancer | Phase 1 | Completed | - | United States, Florida ... More >> H. Lee Moffitt Cancer Center & Research Insitute Tampa, Florida, United States, 33612 Less << |
| NCT00642031 | Hematologic Malignancies|Leuke... More >>mia Less << | PHASE1 | COMPLETED | 2025-10-12 | H. Lee Moffitt Cancer Center, ... More >>Tampa, Florida, 33612, United States|UT MD Anderson Cancer Center, Houston, Texas, 77030, United States Less << |
Tags: Triciribine | API-2 | NSC 154020 | TCN | API2 | API 2 | NSC154020 | NSC 154020 | NSC-154020 | DNA/RNA Synthesis | Akt | HIV | PKB | Protein kinase B | AKT inhibitor | 35943-35-2
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| H261 | In contact with water releases flammable gas |
| H270 | May cause or intensify fire; oxidizer |
| H271 | May cause fire or explosion; strong oxidizer |
| H272 | May intensify fire; oxidizer |
| H280 | Contains gas under pressure; may explode if heated |
| H281 | Contains refrigerated gas; may cause cryogenic burns or injury |
| H290 | May be corrosive to metals |
Health hazards | |
| Code | Phrase |
| H300 | Fatal if swallowed |
| H301 | Toxic if swallowed |
| H302 | Harmful if swallowed |
| H303 | May be harmful if swallowed |
| H304 | May be fatal if swallowed and enters airways |
| H305 | May be harmful if swallowed and enters airways |
| H310 | Fatal in contact with skin |
| H311 | Toxic in contact with skin |
| H312 | Harmful in contact with skin |
| H313 | May be harmful in contact with skin |
| H314 | Causes severe skin burns and eye damage |
| H315 | Causes skin irritation |
| H316 | Causes mild skin irritation |
| H317 | May cause an allergic skin reaction |
| H318 | Causes serious eye damage |
| H319 | Causes serious eye irritation |
| H320 | Causes eye irritation |
| H330 | Fatal if inhaled |
| H331 | Toxic if inhaled |
| H332 | Harmful if inhaled |
| H333 | May be harmful if inhaled |
| H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
| H335 | May cause respiratory irritation |
| H336 | May cause drowsiness or dizziness |
| H340 | May cause genetic defects |
| H341 | Suspected of causing genetic defects |
| H350 | May cause cancer |
| H351 | Suspected of causing cancer |
| H360 | May damage fertility or the unborn child |
| H361 | Suspected of damaging fertility or the unborn child |
| H361d | Suspected of damaging the unborn child |
| H362 | May cause harm to breast-fed children |
| H370 | Causes damage to organs |
| H371 | May cause damage to organs |
| H372 | Causes damage to organs through prolonged or repeated exposure |
| H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
| Code | Phrase |
| H400 | Very toxic to aquatic life |
| H401 | Toxic to aquatic life |
| H402 | Harmful to aquatic life |
| H410 | Very toxic to aquatic life with long-lasting effects |
| H411 | Toxic to aquatic life with long-lasting effects |
| H412 | Harmful to aquatic life with long-lasting effects |
| H413 | May cause long-lasting harmful effects to aquatic life |
| H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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