Structure of Dactolisib
CAS No.: 915019-65-7
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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.
Dactolisib (BEZ235) is an orally active dual inhibitor of pan-class I PI3K and mTOR kinases, with IC50 values of 4 nM, 5 nM, 7 nM, and 75 nM for p110α, p110γ, p110δ, and p110β, respectively, and 20.7 nM for mTOR. Dactolisib inhibits both mTORC1 and mTORC2.
Synonyms: BEZ235; NVP-BEZ235
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CAS No. : | 915019-65-7 |
Formula : | C30H23N5O |
M.W : | 469.54 |
SMILES Code : | CC(C1=CC=C(N(C2=C3C=NC4=CC=C(C5=CC6=CC=CC=C6N=C5)C=C24)C(N3C)=O)C=C1)(C)C#N |
Synonyms : |
BEZ235; NVP-BEZ235
|
MDL No. : | MFCD10565944 |
InChI Key : | JOGKUKXHTYWRGZ-UHFFFAOYSA-N |
Pubchem ID : | 11977753 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
Target |
|
In Vitro:
Concentration | Treated Time | Description | References |
SUM52PE cells | 100 nM | 72 h | Inhibited cell viability, synergistic interaction with the anti-estrogen tamoxifen | PMC7998036 |
SUM52PE cells | 100 nM | 24 h | Inhibited PI3K-AKT-mTOR signaling, downregulated ATF4, MYC, and MTHFD1L expression | PMC7998036 |
HepG2 cells | 0.1 µM | 10 days | Inhibited the PI3K/AKT signaling pathway and blocked the formation of 3D microstructures | PMC9379399 |
MDA-MB-134 cells | 100 nM | 24 h | Dactolisib in combination with tamoxifen significantly inhibits AKT signaling and MTHFD1L expression. | PMC7998036 |
SUM44PE cells | 100 nM | 24 h | Dactolisib in combination with tamoxifen significantly inhibits AKT signaling and MTHFD1L expression. | PMC7998036 |
OSCC cells | 1 µM | 24 h | Inhibit PI3K signaling pathway, reduce cell proliferation | PMC11097543 |
SUM52PE cells | 100 nM | 24 h | Dactolisib inhibits the PI3K-AKT-mTOR signaling pathway, reducing the expression of ATF4, MYC, and MTHFD1L. | PMC7998036 |
H1299 cells | 50 μM | 24 h | To study the effect of Dactolisib on TM4SF1-knocked down H1299 cells, it was found that Dactolisib further down-regulated the DDR1/AKT pathway. | PMC6542073 |
T. brucei bloodstream form | 0.12 µM | 3 days | To evaluate the growth inhibitory effect of Dactolisib on T. brucei bloodstream form, showing an EC50 of 0.12 µM. | PMC7221892 |
L. donovani promastigotes | 0.38 µM | 3 days | To evaluate the growth inhibitory effect of Dactolisib on L. donovani promastigotes, showing an EC50 of 0.38 µM. | PMC7221892 |
THP-1 cells | 0.36 µM | 72 h | To evaluate the inhibitory effect of Dactolisib on intracellular L. donovani, showing an EC50 of 0.36 µM with low toxicity to host cells. | PMC7221892 |
In Vivo:
Administration | Dosage | Frequency | Description | References |
Balb/c nude mice | HGC-27R tumor model | Oral | 45 mg/kg | Once daily for 21 days | To evaluate the antitumor effects of BEZ235 in PTX-resistant gastric cancer models, results showed that BEZ235 significantly inhibited tumor growth by suppressing the PI3K/Akt/mTOR pathway. | PMC5833539 |
BALB/c mice | L. donovani infection model | Oral | 50 mg/kg | Once daily for 5 days | To evaluate the efficacy of Dactolisib in the L. donovani infected mouse model, showing a significant reduction in liver parasite burden with an inhibition rate of 53%. | PMC7221892 |
BALB/c nude mice | OSCC xenograft model | Oral gavage | 10 mg/kg | Once daily for 7-14 days | Evaluate the inhibitory effect of Dactolisib on tumor growth, results showed that Dactolisib significantly inhibited tumor growth | PMC11097543 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT01285466 | Metastatic or Locally Advanced... More >> Solid Tumors Less << | Phase 1 | Completed | - | Belgium ... More >> Novartis Investigative Site Bruxelles, Belgium, 1000 Novartis Investigative Site Bruxelles, Belgium, 1200 Novartis Investigative Site Wilrijk, Belgium, 2610 Germany Novartis Investigative Site Essen, Germany, 45147 Novartis Investigative Site Köln, Germany, 50937 Netherlands Novartis Investigative Site Amsterdam, Netherlands, 1066 CX Spain Novartis Investigative Site Sevilla, Andalucia, Spain, 41013 Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 Switzerland Novartis Investigative Site Chur, Switzerland, 7000 Novartis Investigative Site St. Gallen, Switzerland, 9007 Less << |
NCT02430363 | Glioblastoma | Phase 1 Phase 2 | Unknown | June 2018 | United States, Massachusetts ... More >> Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Texas M D Anderson Cancer Center Houston, Texas, United States, 77030 Belgium UCL- Cliniques Universitaires Saint Luc Brussels, Belgium Germany St Johannes Hospital Duisburg, Germany, 47166 Italy Spedali Civili di Brescia Brescia, Italy IRCCS San Raffaele Milan, Italy Poland Lower-Silesian Oncology Centre Wroclaw, Lower-Silesian, Poland, 53413 Russian Federation Pavlov State Medical University St. Petersburg, Russian Federation, 197089 Spain Hospital Universitario Germans Trias I Pujol Barcelona,, Spain Switzerland Universitätsklinik für Frauenheilkunde Bern, Switzerland Ukraine Regional Cancer Center Dnepropetrovsk, Ukraine, 49000 National Institute of Cancer Kiev, Ukraine, 03035 United Kingdom Royal Victoria Hospital Belfast, Ulster, United Kingdom, BT12 6BA Less << |
NCT01508104 | Cancer | Phase 1 | Terminated(funding) | - | United States, Ohio ... More >> University of Cincinnati Cincinnati, Ohio, United States, 45267-0502 Less << |
NCT00620594 | Breast Cancer|Advanced Solid T... More >>umors|Cowden Syndrome Less << | PHASE1 | COMPLETED | 2013-01-08 | University of California at Lo... More >>s Angeles JonssonComprehensiveCancerCtr, Los Angeles, California, 90095, United States|Yale University School of Medicine YaleCancerCtr-ClinTrialsOffice, New Haven, Connecticut, 06520, United States|Dana Farber Cancer Institute Clinical Trials ProjectManager, Boston, Massachusetts, 02215, United States|Nevada Cancer Institute NVCC - Huntsman, Las Vegas, Nevada, 89135, United States|Cancer Centers of the Carolinas CCC Faris, Greenville, South Carolina, 29605, United States|Sarah Cannon Research Institute Dept.ofSarahCannonCancerCtr(2), Nashville, Tennessee, 37203, United States|Baylor Health Care System/Sammons Cancer Center Baylor- Sammons, Dallas, Texas, 75246, United States|University of Texas/MD Anderson Cancer Center Thoractic Head/Neck Med.Onc(2), Houston, Texas, 77030-4009, United States|Tyler Cancer Center TCC, Tyler, Texas, 75702, United States|Novartis Investigative Site, Essen, 45147, Germany|Novartis Investigative Site, Amsterdam, 1066 CX, Netherlands|Novartis Investigative Site, Barcelona, Catalunya, 08035, Spain|Novartis Investigative Site, Valencia, Comunidad Valenciana, 46009, Spain|Novartis Investigative Site, Valencia, Comunidad Valenciana, 46010, Spain|Novartis Investigative Site, Manchester, M20 9BX, United Kingdom Less << |
NCT01471847 | Locally Advance Breast Cancer ... More >>(LABC) Metastatic Breast Cancer (MBC) Less << | Phase 1 | Completed | - | Spain ... More >> Novartis Investigative Site Madrid, Spain, 28050 United Kingdom Novartis Investigative Site Leicester, United Kingdom, LE1 5WW Novartis Investigative Site Manchester, United Kingdom, M20 2BX Less << |
NCT01300962 | Metastatic Breast Cancer | Phase 1 | Active, not recruiting | December 2018 | United States, North Carolina ... More >> Lineberger Comprehensive Cancer Center Chapel Hill, North Carolina, United States, 27599 Duke Comprehensive Cancer Center Durham, North Carolina, United States, 27710 Less << |
NCT01337765 | Unspecified Adult Solid Tumor,... More >> Protocol Specific Solid Tumor Less << | Phase 1 | Completed | - | United States, Massachusetts ... More >> Massachusetts General Hospital Mass General 2 Boston, Massachusetts, United States, 02114 United States, Texas University of Texas/MD Anderson Cancer Center MD Anderson PSC Houston, Texas, United States, 77030-4009 Australia, Victoria Novartis Investigative Site Parkville, Victoria, Australia, 3050 Canada, Ontario Novartis Investigative Site Toronto, Ontario, Canada, M5G 2M9 France Novartis Investigative Site Villejuif Cedex, France, 94805 Spain Novartis Investigative Site Barcelona, Cataluña, Spain, 08035 Less << |
NCT01288092 | Metastatic Breast Cancer | PHASE2 | WITHDRAWN | - | - |
NCT01195376 | Advanced Solid Tumor | PHASE1 | COMPLETED | 2025-07-13 | Novartis Investigative Site, K... More >>obe-city, Hyogo, 650-0017, Japan|Novartis Investigative Site, Yufu, Oita, 879-5593, Japan Less << |
NCT01634061 | Castration-resistant Prostate ... More >>Cancer Less << | Phase 1 | Completed | - | United States, California ... More >> Cedars Sinai Medical Center SC Los Angeles, California, United States, 90048 United States, New Jersey Hackensack University Medical Center Hackensack Univ Hackensack, New Jersey, United States, 07601 Belgium Novartis Investigative Site Brussels, Belgium, BE-B-1200 Novartis Investigative Site Wilrijk, Belgium, 2610 Canada, British Columbia Novartis Investigative Site Vancouver, British Columbia, Canada, V5Z 4E6 France Novartis Investigative Site Marseille, France, 13273 Novartis Investigative Site Villejuif Cedex, France, 94805 Spain Novartis Investigative Site Barcelona, Catalunya, Spain, 08036 Novartis Investigative Site Madrid, Spain, 28041 United Kingdom Novartis Investigative Site Sutton, United Kingdom, SM2 5PT Less << |
NCT03373903 | Respiratory Tract Infections | Phase 2 | Active, not recruiting | July 2018 | United States, Kansas ... More >> Heartland Research Associates Wichita, Kansas, United States, 67205 Less << |
NCT01495247 | Inoperable Locally Advanced Br... More >>east Cancer Metastatic Breast Cancer (MBC) Less << | Phase 1 Phase 2 | Completed | - | France ... More >> Novartis Investigative Site Dijon Cedex, France, 21034 Novartis Investigative Site Saint-Herblain Cédex, France, 44805 Spain Novartis Investigative Site Hospitalet de LLobregat, Catalunya, Spain, 08907 Less << |
NCT01628913 | Pancreatic Neuroendocrine Tumo... More >>rs (pNET) Less << | Phase 2 | Terminated(This trial was term... More >>inated based on an interim analysis as BEZ235 did not demonstrate a progression free survival advantage to everolimus treatment.) Less << | - | United States, California ... More >> Cedars Sinai Medical Center SC-3 Los Angeles, California, United States, 90048 United States, Colorado University of Colorado Univ Colorado Aurora, Colorado, United States, 80045 United States, Kentucky University of Kentucky Univ Kebtucky Lexington, Kentucky, United States, 40536-0098 United States, New York Montefiore Medical Center SC Bronx, New York, United States, 10467 France Novartis Investigative Site Lyon, France, 69437 Novartis Investigative Site Montpellier Cedex 5, France, 34298 Novartis Investigative Site Paris, France, 75015 Novartis Investigative Site Reims, France, 51092 Novartis Investigative Site Toulouse Cedex 4, France, 31054 Italy Novartis Investigative Site Bologna, BO, Italy, 40138 Novartis Investigative Site Pisa, PI, Italy, 56126 Novartis Investigative Site Roma, RM, Italy, 00189 Netherlands Novartis Investigative Site Amsterdam, Netherlands, 1105 AZ Novartis Investigative Site Groningen, Netherlands, 9713 GZ Russian Federation Novartis Investigative Site Kazan, Russian Federation, 420029 Spain Novartis Investigative Site Sevilla, Andalucia, Spain, 41013 Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 Novartis Investigative Site Hospitalet de LLobregat, Catalunya, Spain, 08907 Novartis Investigative Site Madrid, Spain, 28034 Novartis Investigative Site Madrid, Spain, 28046 Switzerland Novartis Investigative Site Luzern, Switzerland, 6000 United Kingdom Novartis Investigative Site Glasgow, United Kingdom, G11 6NT Novartis Investigative Site London, United Kingdom, NW3 2QG Novartis Investigative Site London, United Kingdom, SE1 9RT Novartis Investigative Site Manchester, United Kingdom, M20 9BX Novartis Investigative Site Sheffield, United Kingdom, S10 2SJ Less << |
NCT01290406 | Endometrial Cancer | PHASE2 | WITHDRAWN | 2025-12-17 | St. Joseph's Hospital & Medica... More >>l Center, Phoenix, Arizona, 85013, United States|Highlands Oncology Group, Fayetteville, Arkansas, 72703, United States|City of Hope Medical center, Duarte, California, 91010, United States|Holy Cross Hospital, Silver Spring, Maryland, 20910-1484, United States|Henry Ford Hospital, Detroit, Michigan, 48202, United States|Morriswon Memorial Hospital, Morristown, New Jersey, 07960, United States|Carolinas Healthcare Systems, Charlotte, North Carolina, 28203, United States|Cancer Centers of North Carolina, Raleigh, North Carolina, 27607, United States|University of Oklahoma Health Sciences Center, Oklahoma City, Oklahoma, 73126-0901, United States|GHS, Danville, Pennsylvania, United States|Sarah Gautam Rau, Nashville, Tennessee, 37203-1197, United States|Texas Oncology, P.A., Austin, Texas, United States|University of Texas Southwestern Medical Center, Dallas, Texas, 75390, United States|STOH, San Antonio, Texas, United States|Pacific Gynecology Specialists, Seattle, Washington, 98104, United States|Cancer Care Northwest, Spokane, Washington, 99202, United States|Novartis Investigative Site, Rio de Janeiro, Brazil|Novartis Investigative Site, Sao Paulo, Brazil|Novartis Investigative Site, Hamilton, Canada|Novartis Investigative Site, Montreal, Canada|Novartis Investigative Site, Toronto, Canada|Novartis Investigative Site, Vancouver, Canada|Novartis Investigative Site, Bordeaux, France|Novartis Investigative Site, Caen Cedex, France|Novartis Investigative Site, La Roche sur Yon Cedex, France|Novartis Investigative Site, Le Mans, France|Novartis Investigative Site, Lyon, France|Novartis Investigative Site, Marseille, France|Novartis Investigative Site, Nice, France|Novartis Investigative Site, Paris, France|Novartis Investigative Site, Saint-Brieuc, France|Novartis Investigative Site, Toulouse Cedex 3, France|Novartis Investigative Site, Berlin, Germany|Novartis Investigative Site, Freiburg, Germany|Novartis Investigative Site, Jena, Germany|Novartis Investigative Site, Koln, Germany|Novartis Investigative Site, Lubeck, Germany|Novartis Investigative Site, Mainz, Germany|Novartis Investigative Site, Munchen, Germany|Novartis Investigative Site, Aviano, Italy|Novartis Investigative Site, Barcelona, Italy|Novartis Investigative Site, Bologna, Italy|Novartis Investigative Site, Brescia, Italy|Novartis Investigative Site, Capmobso, Italy|Novartis Investigative Site, Milano, Italy|Novartis Investigative Site, Modena, Italy|Novartis Investigative Site, Napoli, Italy|Novartis Investigative Site, Roma, Italy|Novartis Investigative Site, Aichi, Japan|Novartis Investigative Site, Hyogo, Japan|Novartis Investigative Site, Tokyo, Japan|Novartis Investigative Site, Sroda Wielkopolska, Poland|Novartis Investigative Site, Warzawa, Poland|Novartis Investigative Site, St. Petersburg, Russian Federation|Novartis Investigative Site, Singapore, Singapore|Novartis Investigative Site, Madrid, Spain|Novartis Investigative Site, Oviedo, Spain|Novartis Investigative Site, Valencia, Spain|Novartis Investigative Site, Istanbul, Turkey Less << |
NCT01482156 | Advanced Solid Tumors ... More >> Metastatic Breast Cancer Metastatic Renal Cell Carcinoma Less << | Phase 1 | Completed | - | United States, Arkansas ... More >> Highlands Oncology Group Dept of Highlands Oncology Grp Fayetteville, Arkansas, United States, 72703 United States, Missouri Washington University School of Medicine Washington University (16) St. Louis, Missouri, United States, 63110 United States, South Carolina Medical University of South Carolina SC Charleston, South Carolina, United States, 29425 Belgium Novartis Investigative Site Wilrijk, Belgium, 2610 France Novartis Investigative Site Bordeaux Cedex, France, 33075 Novartis Investigative Site Montellier cedex 5, France, 34298 Italy Novartis Investigative Site Verona, VR, Italy, 37126 New Zealand Novartis Investigative Site Auckland, New Zealand Spain Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 United Kingdom Novartis Investigative Site High Heaton, Newcastle Upon Tyne, United Kingdom, NE7 7DN Less << |
NCT01756118 | Acute Lymphoblastic Leukemia|L... More >>eukemia, Myelocytic, Acute|Chronic Myelogenous Leukemia With Crisis of Blast Cells Less << | PHASE1 | COMPLETED | 2020-02-07 | Johann Wolfgang Goethe Univers... More >>ity Hospitals, Frankfurt, Hessen, 60590, Germany Less << |
NCT01690871 | Malignant PEComa (Perivascular... More >> Epithelioid Cell Tumors) Less << | PHASE2 | WITHDRAWN | 2025-01-15 | Novartis Investigative Site, B... More >>arcelona, Catalu?a, 08025, Spain Less << |
NCT01453595 | Renal Cancer | PHASE1|PHASE2 | TERMINATED | 2025-04-14 | Memorial Sloan Kettering Cance... More >>r Center, New York, New York, 10065, United States Less << |
NCT01628913 | - | Terminated(This trial was term... More >>inated based on an interim analysis as BEZ235 did not demonstrate a progression free survival advantage to everolimus treatment.) Less << | - | - | |
NCT01658436 | Pancreatic Neuroendocrine Tumo... More >>rs (pNET) Less << | Phase 2 | Completed | - | United States, Indiana ... More >> Indiana University SC Indianapolis, Indiana, United States, 46202 United States, Massachusetts Dana Farber Cancer Institute GastrointestionalCancer Clinic Boston, Massachusetts, United States, 02215 United States, New York Montefiore Medical Center SC-2 Bronx, New York, United States, 10467 United States, Ohio Ohio State Comprehensive Cancer Center/James Cancer Hospital SC Columbus, Ohio, United States, 43210 Austria Novartis Investigative Site Wien, Austria, A-1090 Belgium Novartis Investigative Site Leuven, Belgium, 3000 France Novartis Investigative Site Lyon, France, 69437 Novartis Investigative Site Villejuif Cedex, France, 94805 Germany Novartis Investigative Site Essen, Germany, 45147 Italy Novartis Investigative Site Firenze, FI, Italy, 50134 Novartis Investigative Site Milano, MI, Italy, 20133 Novartis Investigative Site Milano, MI, Italy, 20141 Netherlands Novartis Investigative Site Rotterdam, Netherlands, 3015 CE Spain Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 Novartis Investigative Site Hospitalet de LLobregat, Catalunya, Spain, 08907 Novartis Investigative Site Madrid, Spain, 28041 United Kingdom Novartis Investigative Site Manchester, United Kingdom, M20 4BX Less << |
NCT01453595 | Renal Cancer | PHASE1|PHASE2 | TERMINATED | 2025-04-14 | Memorial Sloan Kettering Cance... More >>r Center, New York, New York, 10065, United States Less << |
NCT01717898 | Castrate-resistant Prostate Ca... More >>ncer Less << | Phase 1 Phase 2 | Terminated(Dose limiting toxic... More >>ities on lowest dose level) Less << | - | United States, California ... More >> University of California, San Francisco San Francisco, California, United States, 94115 Less << |
NCT01658436 | - | Completed | - | - | |
NCT01717898 | - | Terminated(Dose limiting toxic... More >>ities on lowest dose level) Less << | - | - | |
NCT01856101 | Carcinoma Transitional Cell | PHASE2 | TERMINATED | 2025-01-14 | Clinique Saint-Pierre à Ottign... More >>ies, Ottignies, Brabant Wallon, 1340, Belgium|Epicura- RHMS Baudour, Baudour, Hainaut, 7331, Belgium|Grand H?pital de Charleroi, Charleroi, Hainaut, 6000, Belgium|H?pital de Jolimont, Haine-Saint-Paul, Hainaut, 7100, Belgium|Centre Hospitalier Wallonie Picarde, Tournai, Hainaut, 7500, Belgium|CHU de Liège site du Sart Tilman, Liège 1, Liège, 4000, Belgium|Clinique du Sud Luxembourg, Arlon, Luxembourg, 6700, Belgium|CHU de Mont-Godinne, Yvoir, Namur, 5530, Belgium|Cliniques universitaires Saint-Luc, Brussel, 1200, Belgium|Universitair Ziekenhuis Gent, Gent, 9000, Belgium|Clinique et Maternité Ste Elisabeth, Namur, 5000, Belgium|Centre Hospitalier de Luxembourg, Luxembourg, Grand-Duché De Luxembourg, 1210, Luxembourg Less << |
NCT01248494 | Metastatic Breast Cancer | Phase 1 | Completed | - | United States, Alabama ... More >> University of Alabama Birmingham, Alabama, United States United States, Massachusetts Massachusetts General Hospital, Dana Farber Cancer Center Boston, Massachusetts, United States, 02114 United States, New York Columbia University Medical Center New York City, New York, United States United States, Tennessee Vanderbilt Cool Springs Nashville, Tennessee, United States, 37067 Vanderbilt Breast Center One Hundred Oaks Nashville, Tennessee, United States, 37204 Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232 Less << |
NCT01343498 | Malignant Solid Tumour | PHASE1 | COMPLETED | 2025-01-14 | Oklahoma University, Oklahoma ... More >>City, Oklahoma, 71304, United States|Tennessee Oncology, Nashville, Tennessee, 37203, United States Less << |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.13mL 0.43mL 0.21mL |
10.65mL 2.13mL 1.06mL |
21.30mL 4.26mL 2.13mL |