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Chemical Structure| 1211441-98-3 Chemical Structure| 1211441-98-3

Structure of Ribociclib
CAS No.: 1211441-98-3

Chemical Structure| 1211441-98-3

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Ribociclib (LEE01) demonstrates high specificity as a CDK4/6 inhibitor, displaying IC50 values of 10 nM and 39 nM, respectively, while being over 1,000-fold less potent against the cyclin B/CDK1 complex.

Synonyms: LEE011

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Product Citations

Product Citations

Adam M. Weiss ; Marcos A. Lopez II ; Matthew G. Rosenberger ; Jeremiah Y. Kim ; Jingjing Shen ; Qing Chen , et al.

Abstract: Several FDA-approved adjuvants signal through the NLRP3 inflammasome and IL-1β release. Identifying small molecules that induce IL-1β release could allow targeted delivery and structure−function optimization, thereby improving safety and efficacy of next-generation adjuvants. In this work, we leverage our existing high throughput data set to identify small molecules that induce IL-1β release. We find that induces IL-1β release when coadministered with a TLR4 agonist in an NLRP3- and caspase-dependent fashion. was formulated with a TLR4 agonist into liposomes, which were used as an adjuvant in an ovalbumin prophylactic vaccine model. The liposomes induced antigen-specific immunity in an IL-1 receptor-dependent fashion. Furthermore, the liposomes were coadministered with a tumor antigen and used in a therapeutic cancer vaccine, where they facilitated rejection of E.G7-OVA tumors. While further chemical optimization of the scaffold is needed, this study provides proof-of-concept for its use as an IL-1 producing adjuvant in various immunotherapeutic contexts.

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Product Details of Ribociclib

CAS No. :1211441-98-3
Formula : C23H30N8O
M.W : 434.54
SMILES Code : O=C(C1=CC2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5)N(C)C
Synonyms :
LEE011
MDL No. :MFCD27976795
InChI Key :RHXHGRAEPCAFML-UHFFFAOYSA-N
Pubchem ID :44631912

Safety of Ribociclib

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

Related Pathways of Ribociclib

Hedgehog

Isoform Comparison

Biological Activity

Target
  • CDK4

    CDK4, IC50:10 nM

  • CDK6

    CDK6, IC50:39 nM

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02431481 Normal Renal Function|Impaired... More >> Renal Function Less << PHASE1 COMPLETED 2018-05-11 DaVita Clinical Research, Minn... More >>eapolis, Minnesota, 55404, United States|Novartis Investigative Site, Sofia, 1612, Bulgaria|Novartis Investigative Site, Praha 4, Czech Republic, 140 59, Czechia|Novartis Investigative Site, Berlin, 14050, Germany Less <<
NCT02388620 Normal Hepatic Function|Impair... More >>ed Hepatic Function Less << PHASE1 COMPLETED 2017-01-09 Anaheim Clinical Trials, Anahe... More >>im, California, 92801, United States|University of Miami, Coral Gables, Florida, 33124, United States|Orlando Clinical Research Center, Orlando, Florida, 32809, United States Less <<
NCT05038631 Breast Cancer AVAILABLE - -
NCT03956654 Breast Cancer COMPLETED 2024-06-30 UZ Gasthuisberg Leuven, Leuven... More >>, B-3000, Belgium Less <<
NCT04657679 Breast Cancer PHASE4 TERMINATED 2023-10-30 MedStar Georgetown University ... More >>Hospital, Washington, District of Columbia, 20007, United States|Medstar Washington Hospital Center, Washington, District of Columbia, 20010, United States|Tufts Medical Center, Boston, Massachusetts, 02111, United States Less <<
NCT03096912 Liposarcomas, Dedifferentiated... More >>|Liposarcoma - Well Differentiated|Liposarcoma; Mixed Type|Soft-Tissue Sarcoma Less << PHASE2 UNKNOWN 2025-04-20 Assaf Harofeh Medical Center, ... More >>Be'er Ya'aqov, 70300, Israel Less <<
NCT06587789 Breast Cancer RECRUITING 2027-01-01 Second Affiliated Hospital of ... More >>Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310009, China Less <<
NCT05452213 Breast Cancer|Breast Neoplasms... More >>|Breast Neoplasm Female|Breast Cancer Female|HER2-negative Breast Cancer|Hormone Receptor-positive Breast Cancer|Advanced Breast Cancer Less << PHASE4 RECRUITING 2025-10-26 Department of Gynecology and O... More >>bstetrics, Erlangen University Hospital, Erlangen, Bavaria, 91054, Germany|Department of Gynecology and Obstetrics, University Medicine Mainz, Mainz, Hesse, 55131, Germany|Department for Gynecology and Obstetrics, Marienhospital Bottrop gGmbH, Bottrop, North Rhine-Westphalia, 46236, Germany|Klinikum St Marien Amberg, Amberg, 92224, Germany|Onkologie Aschaffenburg, H?mato-Onkologische Schwerpunktpraxis am Klinikum Aschaffenburg, Aschaffenburg, 63739, Germany|Klinik für H?matologie und Onkologie, Uniklinik Augsburg, Augsburg, 86156, Germany|University Hospital Augsburg, Augsburg, 86156, Germany|Frauenklinik des Klinikums Bamberg, Bamberg, 96049, Germany|MediOnko GbR, Berlin, 10367, Germany|HELIOS Klinikum Berlin-Buch, Berlin, 13125, Germany|Zentrum für ambulante H?matologie und Onkologie (ZAHO) an der Robert-Janker-Klinik, Bonn, 53129, Germany|Klinik für Gyn?kologie, Gyn?koonkologie und Senologie Klinikum Bremen-Mitte, Bremen, 28205, Germany|Klinikum Chemnitz gGmbH, Klinik für Frauenheilkunde und Geburtshilfe, Chemnitz, 09116, Germany|Kliniken Der Stadt K?ln gGmbH, Cologne, 51067, Germany|Carl-Thiem-Klinikum Cottbus, Cottbus, 03048, Germany|Staedtisches Klinikum Dessau, Gynecology and Obstetrics, Dessau, 06847, Germany|Universit?ts-Frauenklinik Carl Gustav Carus Universit?t Dresden, Dresden, 01307, Germany|Universitaetsklinikum Duesseldorf A?R, Duesseldorf, 40225, Germany|Universitaetsklinikum Essen A?R, Gynecology and Obstetrics, Essen, 45147, Germany|Klinikum Esslingen GmbH, Esslingen, 73730, Germany|Agaplesion Frankfurter Diakonie Kliniken gGmbH, Gynecology and Obstetrics, Frankfurt Am Main, 60431, Germany|Universit?ts-Frauenklinik Frankfurt, Frankfurt am Main, 60596, Germany|Universit?ts-Frauenklinik Freiburg, Freiburg, 79106, Germany|Medizinisches Versorgungszentrum Onkologie Georgsmarienhütte und Bramsche, Georgsmarienhütte, 49124, Germany|Universit?ts-Frauenklinik Hamburg-Eppendorf, Hamburg, 20246, Germany|Mammazentrum Hamburg am Krankenhaus Jerusalem, Hamburg, 20357, Germany|Nationales Centrum für Tumorerkrankungen, Universit?tsklinikum Heidelberg Abteilung für Gyn?kologie und Geburtshilfe, Heidelberg, 69120, Germany|Frauenklinik, SLK-Kliniken Heilbronn GmbH, Heilbronn, 74078, Germany|Staedtisches Klinikum Karlsruhe gGmbH, Gynecology and Obstetrics, Karlsruhe, 76133, Germany|University Medical Centre Schleswig-Holstein, Gynecology and Obstetrics, Kiel, 24105, Germany|ZAGO-Zentrum für ambulante gyn?kologische Onkologie, Krefeld, 47805, Germany|Klinikum Kulmbach, Kulmbach, 95326, Germany|VK&K Studienzentrum Landshut am Lakumed Klinikum Landshut-Achdorf, Landshut, 84036, Germany|Praxis Dr. Müller MVM GmbH, Studienzentrum UnterEms, Leer, 26789, Germany|Universit?ts-Frauenklinik Leipzig, Leipzig, 04103, Germany|H?matologie Onkologie Gemeinschaftspraxis Pasing, Munich, 81241, Germany|Ev. Krankenhaus Bethesda M?nchengladbach, M?nchengladbach, 41061, Germany|MVZ Nordhausen gGmbH, Nordhausen, 99734, Germany|Klinikum Nürnberg, Nuremberg, 90419, Germany|Frauenklinik, Medius Klinik Nürtingen, Nürtingen, 72622, Germany|Gemeinschaftspraxis für H?matologie und Onkologie GbR, Ravensburg, 88212, Germany|Frauenklinik, Diakoniekrankenhaus Rotenburg, Rotenburg, 27356, Germany|Leopoldina Krankenhaus der Stadt Schweinfurt gGmbH, Schweinfurt, 97422, Germany|Schwerpunktpraxis für H?matologie, Onkologie und Magen-Darm Diagnostik, Singen, 78224, Germany|Onkologische Schwerpunktpraxis Speyer, Speyer, 61346, Germany|Klinikum Stuttgart, Stuttgart, 70174, Germany|Onkologie Rheinsieg, Praxisnetzwerk H?matologie und internistische Onkologie, Troisdorf, 53840, Germany|Universitaetsklinikum Tuebingen, Tuebingen, 72076, Germany|Universit?ts-Frauenklinik Ulm, Ulm, 89075, Germany|MVZ Nordoberpfalz, Weiden, 92637, Germany|Medizinische Studiengesellschaft Nord-West GmbH, Westerstede, 26655, Germany|Rems-Murr Kliniken Winnenden, Winnenden, 71364, Germany Less <<
NCT03179956 Squamous Cell Carcinoma of the... More >> Head and Neck Less << EARLY_PHASE1 TERMINATED 2019-01-10 Fox Chase Cancer Center, Phila... More >>delphia, Pennsylvania, 19111, United States Less <<
NCT02187783 Tumors With CDK4/6 Pathway Act... More >>ivation Less << PHASE2 COMPLETED 2018-01-17 University of Alabama at Birmi... More >>ngham, Birmingham, Alabama, 35249, United States|Alaska Clinical Research, Anchorage, Alaska, 99503, United States|Arizona Oncology Associates Dept. Of Onc., Phoenix, Arizona, United States|University of Arkansas/ Arkansas Cancer Research Center UA Medical Sciences, Little Rock, Arkansas, 72205, United States|PCR Oncology, Pismo Beach, California, 93449, United States|University of California Davis Cancer Center UC Davis Cancer (3), Sacramento, California, 95817, United States|Sarah Cannon Research Institute, Denver, Colorado, 80218, United States|Danbury Hospital, Danbury, Connecticut, 06810, United States|Yale University School of Medicine Smilow Cancer Hospital, New Haven, Connecticut, 06520, United States|Whittingham Cancer Center Norwalk Hospital, Norwalk, Connecticut, 06856, United States|Stamford Hospital Med. Oncology Hematology Res., Stamford, Connecticut, 06902, United States|Florida Hospital Cancer Institute, Orlando, Florida, 32804, United States|NorthWest Georgia Oncology Centers NW Georgia Oncology, Marietta, Georgia, 30060, United States|Harbin Clinic Medical Oncology Clin. Res., Rome, Georgia, 30165, United States|Queen's Medical Center Queens Cancer Center, Honolulu, Hawaii, 96817, United States|Northwestern Medicine Developmental Therapeutics Institute, Chicago, Illinois, 60611, United States|Indiana University Indiana Univ. - Purdue Univ., Indianapolis, Indiana, 46202, United States|Northern Indiana Cancer Research Consortium No. Indiana Cancer Res., South Bend, Indiana, 46617, United States|University of Iowa Hospitals & Clinics Regulatory Contact 2, Iowa City, Iowa, 52242, United States|New England Cancer Specialists, Scarborough, Maine, 04074, United States|St. Agnes Hospital St. Agnes Hospital (2), Baltimore, Maryland, 21229, United States|Michigan Medicine University of Michigan Int. Medicine Oncology, Ann Arbor, Michigan, 48109 5271, United States|Cancer and Hematology Centers of West Michigan Dept. of Oncology, Grand Rapids, Michigan, 49546, United States|Saint Luke's Hospital/Marion Bloch Neuroscience Institute St. Luke's Hospital (4), Kansas City, Missouri, 64111, United States|Research Medical Center Research Med Center (2), Kansas City, Missouri, 64132, United States|Comprehensive Cancer Centers of Nevada CCC of Nevada- Southwest (2), Las Vegas, Nevada, 89109, United States|Cooper Health System Cooper Health System (5), Camden, New Jersey, 08103, United States|Rutgers Cancer Institute of New Jersey, New Brunswick, New Jersey, 08903, United States|New Mexico Cancer Care Alliance, Albuquerque, New Mexico, 87106, United States|Cancer Center at Presbyterian, Albuquerque, New Mexico, United States|Broome Oncology Broome Oncology (2), Johnson City, New York, 13790, United States|University of N C at Chapel Hill Physician Office Building, Chapel Hill, North Carolina, 27599-7600, United States|Carolina Oncology Specialists, PC, Hickory, North Carolina, 28602, United States|Wake Forest University Baptist Medical Center, Winston-Salem, North Carolina, 27157, United States|Oncology Hematology Care Inc Oncology Hematology Care 2, Cincinnati, Ohio, 45242, United States|Cleveland Clinic Foundation Taussig Cancer Institute, Cleveland, Ohio, 44195, United States|Ohio State University Medical Center Comprehensive Cancer Center, Columbus, Ohio, 43221, United States|Oregon Health and Science University Oregon Health & Science U (56), Portland, Oregon, 97239, United States|Salem Health, Salem, Oregon, 97309, United States|Fox Chase Cancer Center Dept of Medical Oncology, Philadelphia, Pennsylvania, 19111, United States|Rhode Island Hospital Rhode Island Hosp. (2), Providence, Rhode Island, 02903, United States|Greenville Health System ITOR - Cancer Institute, Greenville, South Carolina, 29615, United States|Sanford University of South Dakota Medical Center Sanford Health, Sioux Falls, South Dakota, 57104, United States|Chattanooga Oncology and Hematology Assoicates, PC Chattanooga Oncology, Chattanooga, Tennessee, 37404, United States|The West Clinic Dept. of the West Clinic, Memphis, Tennessee, 38120, United States|Tennessee Oncology Tennessee Oncology (3), Nashville, Tennessee, 37203, United States|Coastal Bend Cancer Center, Corpus Christi, Texas, 78404, United States|Oncology Consultants Oncology Group, Houston, Texas, 77024, United States|MD Anderson Cancer Center/University of Texas MD Anderson Cancer Center (3), Houston, Texas, 77030, United States|University of Texas Health Science Center at San Antonio Cancer Therapy & Research Ctr., San Antonio, Texas, 78229, United States|Intermountain Medical Center Intermountain Healthcare, Murray, Utah, 84157, United States|Utah Cancer Specialists Utah Cancer Specialists (11), Salt Lake City, Utah, 84106, United States|Shenandoah Oncology Shenadoah Oncology (2), Winchester, Virginia, 22601, United States|Kadlec Clinic Hematology and Oncology Kadlec Clinic Hematology & Onc, Kennewick, Washington, 99336, United States|Vista Oncology Inc. PS, Olympia, Washington, 98502, United States|Multicare Research Institute, Tacoma, Washington, 98405, United States|Northwest Medical Specialties Rainier Physicians, PC, Tacoma, Washington, 98405, United States|Providence St. Mary Regional Cancer Center, Walla Walla, Washington, 98057, United States|Wenatchee Valley Medical Center Wenatchee Valley, Wenatchee, Washington, 98801, United States|Aurora Research Institute Aurora Health Care, Milwaukee, Wisconsin, 53226, United States|Medical College of Wisconsin Cancer Center, Milwaukee, Wisconsin, 53226, United States Less <<
NCT02934568 Continued Access to Study Trea... More >>tment(s), Cancers With a Mass, Bulky Tumor, Nodule, Lump, Advanced Cancer, Advanced Solid Tumors, Advanced Solid Malignancies Less << PHASE2 RECRUITING 2026-09-01 University Of Alabama At Birmi... More >>ngham, Birmingham, Alabama, 35294-3300, United States|Dana Farber Cancer Institute Main Site, Boston, Massachusetts, 02215, United States|The Regents of the University of Michigan, Ann Arbor, Michigan, 48109-5930, United States|Broome Oncology SC-2, Johnson City, New York, 13790, United States|St Jude Childrens Research Hospital, Memphis, Tennessee, 38105, United States|Novartis Investigative Site, Lyon, 69373, France|Novartis Investigative Site, Villejuif, 94800, France|Novartis Investigative Site, Singapore, 119228, Singapore|Novartis Investigative Site, Barcelona, Catalunya, 08035, Spain|Novartis Investigative Site, Madrid, 28041, Spain|Novartis Investigative Site, Madrid, 28050, Spain|Novartis Investigative Site, Tainan, 70403, Taiwan|Novartis Investigative Site, Taipei, 10002, Taiwan Less <<
NCT01237236 Advanced Solid Tumor|Lymphomas PHASE1 COMPLETED 2017-03-09 Dana Farber Cancer Institute D... More >>FCI, Boston, Massachusetts, 02215, United States|University of Michigan Comprehensive Cancer Center SC, Ann Arbor, Michigan, +1 48109 0944, United States|Memorial Sloan Kettering MSKCC (2), New York, New York, 10017, United States|Sarah Cannon Research Institute DeptofSarahCannonRes.Inst. (2), Nashville, Tennessee, 37203, United States|Novartis Investigative Site, Lyon Cedex, 69373, France|Novartis Investigative Site, Villejuif Cedex, 94805, France|Novartis Investigative Site, Utrecht, 3584CX, Netherlands Less <<
NCT02429089 Squamous Cell Carcinoma of the... More >> Head and Neck Less << PHASE1 TERMINATED 2018-09-01 Grand H?pital de Charleroi sit... More >>e Notre Dame, Charleroi, Hainaut, 6000, Belgium|H?pital de Jolimont, Haine-Saint-Paul, Hainaut, 7100, Belgium|Cliniques universitaires Saint-Luc, Brussel, 1200, Belgium|Universitair Ziekenhuis Gent, Gent, 9000, Belgium|Clinique et Maternité Sainte-Elisabeth, Namur, 5000, Belgium Less <<
NCT05569187 Breast Cancer COMPLETED 2021-10-29 Novartis Investigative Site, S... More >>ao Paulo, SP, 01317 000, Brazil Less <<
NCT01747876 Malignant Rhabdoid Tumors (MRT... More >>)|Neuroblastoma Less << PHASE1 TERMINATED 2017-06-29 UCSF Medical Center Dept of Pe... More >>diatic Oncology, San Francisco, California, 94143, United States|Childrens Healthcare of Atlanta Dept of Oncology, Atlanta, Georgia, 30342, United States|Dana Farber Cancer Institute SC-7, Boston, Massachusetts, 02215, United States|Memorial Sloan Kettering Dept of Onc, New York, New York, 10017, United States|Cincinnati Children's Hospital Medical Center Dept of Oncology, Cincinnati, Ohio, 45229-3039, United States|St Jude s Childrens Research Hospital Dept of Oncology, Memphis, Tennessee, 38105-2794, United States|Novartis Investigative Site, Perth, Western Australia, 6840, Australia|Novartis Investigative Site, Lyon Cedex, 69373, France|Novartis Investigative Site, Paris, 75231, France|Novartis Investigative Site, Villejuif Cedex, 94805, France|Novartis Investigative Site, Koeln, Nordrhein-Westfalen, 50937, Germany|Novartis Investigative Site, Augsburg, 86156, Germany|Novartis Investigative Site, Sutton, Surrey, SM2 5PT, United Kingdom Less <<
NCT02345824 Glioblastoma|Glioma PHASE1 UNKNOWN 2025-01-20 University of Virginia Health ... More >>System, Charlottesville, Virginia, 22908, United States Less <<
NCT02933736 Glioblastoma Multiforme|Mening... More >>ioma Less << EARLY_PHASE1 ACTIVE_NOT_RECRUITING 2025-01-25 Barrow Brain and Spine, Phoeni... More >>x, Arizona, 85013, United States Less <<
NCT02607124 High Grade Glioma|Diffuse Intr... More >>insic Pontine Glioma|Bithalamic High Grade Glioma Less << PHASE1|PHASE2 TERMINATED 2025-08-18 Cincinnati Children's Hospital... More >> Medical Center, Cincinnati, Ohio, 45229, United States Less <<
NCT01898845 Advanced Solid Tumors PHASE1 COMPLETED 2025-01-15 Novartis Investigative Site, K... More >>ashiwa, Chiba, Japan|Novartis Investigative Site, Chuo-ku, Tokyo, Japan Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.51mL

2.30mL

1.15mL

23.01mL

4.60mL

2.30mL

References

 

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