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Chemical Structure| 1799328-86-1 Chemical Structure| 1799328-86-1

Structure of Tolinapant
CAS No.: 1799328-86-1

Chemical Structure| 1799328-86-1

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An orally bioavailable, non-peptidomimetic antagonist of both X chromosome-linked inhibitor of apoptosis protein (XIAP) and cellular IAP 1 (cIAP1), with potential antineoplastic and pro-apoptotic activities.

Synonyms: ASTX660

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Product Details of Tolinapant

CAS No. :1799328-86-1
Formula : C30H42FN5O3
M.W : 539.68
SMILES Code : C[C@H]1N(C[C@@H]2N(CC(N3CC(C)(C)C4=NC(CO)=C(CC5=CC=C(F)C=C5)C=C43)=O)C[C@@H](C)NC2)CCOC1
Synonyms :
ASTX660
MDL No. :MFCD31619274
InChI Key :YCXOHEXZVKOGEV-DNRQZRRGSA-N
Pubchem ID :118169620

Safety of Tolinapant

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 (Human) 0.014-10 μM 48-80 hours To evaluate the immune-mediated killing effects of Tolinapant on A549 cells. Results showed that Tolinapant significantly increased apoptosis of A549 cells in the presence of activated PBMCs. PMC8945623
HH (Human) 0.001-10 μM 72 hours To evaluate the cytotoxic effects of Tolinapant on the human TCL cell line HH. Results showed that Tolinapant had minimal impact on HH cell viability within 72 hours, but the effect was enhanced in the presence of TNF-α. PMC8945623
BW5147.G.1.4 (Mouse) 0.001-10 μM 72 hours To evaluate the cytotoxic effects of Tolinapant on the mouse TCL cell line BW5147.G.1.4. Results showed that Tolinapant significantly reduced cell viability within 72 hours, especially in the presence of TNF-α. PMC8945623
MDA-MB-231 cells 4.4 nM (GI50) Evaluate the inhibitory effect of Tolinapant on MDA-MB-231 cells PMC11503241

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice BW5147 syngeneic model Oral 25 mg/kg Once daily for 15 days To evaluate the antitumor effects of Tolinapant in the BW5147 syngeneic model. Results showed that Tolinapant treatment led to complete tumor regression, and no tumor recurrence was observed within 30 days after treatment cessation. PMC8945623
Mice MDA-MB-231 xenograft models Oral 30 mg/kg Once daily Evaluate the efficacy of Tolinapant in MDA-MB-231 xenograft models PMC11503241

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02503423 Solid Tumors|Lymphoma PHASE1|PHASE2 ACTIVE_NOT_RECRUITING 2025-12-25 University of Alabama at Birmi... More >>ngham, Birmingham, Alabama, 35294, United States|HonorHealth Research Institute, Scottsdale, Arizona, 852558, United States|USC/Norris Comprehensive Cancer Center, Los Angeles, California, 90033, United States|Cedars-Sinai Medical Center, Los Angeles, California, 90048, United States|UC Davis Medical Center, Sacramento, California, 95817, United States|Simlow Cancer Hospital at Yale, New Haven, Connecticut, 06510, United States|Emory University winship Cancer Institute, Atlanta, Georgia, 30322, United States|Robert H. Lurie Comprehensive Cancer Center of Northwestern University, Chicago, Illinois, 60611, United States|The Sidney Kimmel Comprehensive Cancer Center at John Hopkins, Baltimore, Maryland, 21287, United States|Tufts Medical Center, Boston, Massachusetts, 02111, United States|Dana-Farber Cancer Institute, Boston, Massachusetts, 02215, United States|University of Michigan, Ann Arbor, Michigan, 48109, United States|Dartmouth-Hitchcock Medical Center (DHMC), Lebanon, New Hampshire, 03766, United States|Summit Medical Group - Florham Park Campus/Atlantic Health, Florham Park, New Jersey, 07932, United States|Roswell Park Cancer Institute, Buffalo, New York, 14263, United States|New York University Langone Medical Center, New York, New York, 10016, United States|New York Presbyterian Hospital Columbia University Medical Center, New York, New York, 10019, United States|Icahn School of Medicine at Mount Sinai, New York, New York, 10029, United States|Rochester Skin Lymphoma Medical Group, Rochester, New York, 14450, United States|Wake Forest Baptist Health, Winston-Salem, North Carolina, 27157, United States|The Ohio State University and Wexner Medical Center, James Cancer Hospital, Columbus, Ohio, 43210, United States|University of Oklahoma Stephenson Cancer Center, Oklahoma City, Oklahoma, 73104, United States|Oregon Health and Science University, Portland, Oregon, 97239, United States|West Penn Hospital, Pittsburgh, Pennsylvania, 15224, United States|Hollings Cancer Center, Charleston, South Carolina, 29425, United States|Vanderbilt Ingram Cancer Center, Nashville, Tennessee, 37212, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States|CliniCore Texas, Houston, Texas, 77079, United States|START- South Texas Accelerated Research Therapeutics, San Antonio, Texas, 78229, United States|Virgina Commonwealth University, Richmond, Virginia, 23298, United States|University of Washington, Seattle Cancer Care Alliance, Seattle, Washington, 98109, United States|Centre Hospitalier Universitaire Universite Catholique de Louvain - Site Godinne, Yvoir, Namur, B-5530, Belgium|Universitair Ziekenhuis Gent, Gent, Oost-Vlaanderen, 9000, Belgium|Intitut Jules Boredt, Bruxelles, 1000, Belgium|Tom Baker Cancer Centre, Calgary, Alberta, Canada|British Columbia Cancer Agency, Vancouver, British Columbia, V5Z 4E6, Canada|Cancer Care Manitoba, Winnipeg, Manitoba, R3E 0V9, Canada|Nova Scotia Health Athority-Qeii HSC, Halifax, Nova Scotia, B3H 2Y9, Canada|Sunnybrook Hospital, Toronto, Ontario, M4N 3M5, Canada|Princess Margaret Cancer Centre, Toronto, Ontario, M56 2M9, Canada|Jewish General Hospital, Montréal, Quebec, H3T 1E2, Canada|Gustave Roussy Cancer Campus (IGR), Villejuif, Cedex, 94805, France|Centre Hospitalier Lyon Sud, Pierre-Bénite, Lyon, 69310, France|Institut Bergonié, Unicancer, Bordeaux, 33000, France|Centre Antoine Lacassagne, Oncologie Médicale, Nice, 06189, France|Centre Henri Becquerel, Hematology, Rouen, 1,76-38, France|Institut Universitaire du Cancer - Oncop?le, Department d'Hématologie, Toulouse Cedex 9, 31059, France|CRU de Tours - H?pital Bretonneau, Hématologie -Thérapy Cellulaire, Tours, 37044, France|Semmelweis Egyetem - I. sz. Belgyógyászati Klinika, Budapest, 1083, Hungary|Debreceni Egyetem Klinikai K?zpont, Debrecen, 4032, Hungary|Szabolcs-Szatmár-Bereg Megyei Kórházak és Egyetemi Oktatókórház, Nyíregyháza, Hungary|Azienda Ospedaliero-Universitaria di Bologna Policlinico Sant Orsola-Malpighi, Bologna, 40138, Italy|Azienda Socio Sanitaria Territoriale degli Spedali Civili di Brescia, Brescia, 25123, Italy|Instituto Europeo di Oncologia, Milan, Italy|Azienda Socio Santaria Territoriale Monza- Osperdale San Gerado, Monza, Italy|Institut Catala d'Oncologia, Girona, Giona, Spain|imCORE - Clínica Universidad de Navarra, Pamplona, Navarra, 31008, Spain|Hospital Universitario Fundacion Jimenez Diaz Preview, Madrid, 28040, Spain|Hospital Universitario 12 de Octubre, Madrid, 28041, Spain|University Hospitals of Leicester NHS Trust, Leicester, East Midlands, LE1 5WW, United Kingdom|University Hospital Southhampton NHS Foundation Trust - Somers Cancer Research, Southampton, Hampshire, SO16 6YD, United Kingdom|Churchill Hospital, Oxford University Hospital NHS Trust, Oxford, Oxfordshire, OX3 7LE, United Kingdom|The Royal Marsden NHS Foundation Trust, Sutton, Surrey, SM2 5PT, United Kingdom|University Hospitals Birmingham NHS Foundation Trust, Queen Elizabeth Hospital, Birmingham, B15 2TH, United Kingdom|Beatson Cancer Center and University of Glasgow, Glasgow, G12 0XL, United Kingdom|University College London Hospitals NHS Foundation Trust, London, NW1 2PG, United Kingdom|Guy's and Saint Thomas' NHS Foundation Trust, London, SE1 9RT, United Kingdom|The Christie NHS Foundation Trust, Christie Hospital, Manchester, M20 4BX, United Kingdom Less <<
NCT04479800 Healthy Volunteer PHASE1 COMPLETED 2020-08-25 Worldwide Clinical Trials, San... More >> Antonio, Texas, 78217, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.19mL

9.26mL

1.85mL

0.93mL

18.53mL

3.71mL

1.85mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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