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Chemical Structure| 915019-65-7 Chemical Structure| 915019-65-7

Structure of Dactolisib
CAS No.: 915019-65-7

Chemical Structure| 915019-65-7

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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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Product Details of Dactolisib

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

Safety of Dactolisib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Dactolisib

DNA
PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    p110γ, IC50:5 nM

  • p110β

    p110β, IC50:75 nM

  • p110α

    p110α1, IC50:4 nM

  • p110δ

    p110δ, IC50:7 nM

In Vitro:

Cell Line
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:

Species
Animal Model
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 <<

Protocol

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

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