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Chemical Structure| 1129403-56-0 Chemical Structure| 1129403-56-0

Structure of Amcasertib
CAS No.: 1129403-56-0

Chemical Structure| 1129403-56-0

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Amcasertib is an inhibitor of cancer stem cells (CSCs) with growth inhibition IC50s of 100-250 nM for HT-29 and MDA-MB-231 cancer cells. It also inhibits EGFR, C-MET, HER2, and PDGFRα in vitro without reducing global tyrosine kinase activity.

Synonyms: BBI503

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Product Details of Amcasertib

CAS No. :1129403-56-0
Formula : C31H33N5O2S
M.W : 539.69
SMILES Code : O=C(C1=C(C)NC(/C=C2C(NC3=C/2C=C(C4=CSC(C5=CC=CC=C5)=N4)C=C3)=O)=C1C)NCCN(CC)CC
Synonyms :
BBI503
MDL No. :MFCD30489231

Safety of Amcasertib

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
PC-9/GR cells 0.1 and 1 μM 48 hours Inhibited the NANOG and CD133 expression, and reduced cell viability PMC7441324
PC-9/GR cells 0.1 and 1 μM 48 hours Inhibited the NANOG and CD133 expression, and reduced cell viability PMC10506422

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02232646 Urologic Malignancies|Renal Ce... More >>ll Carcinoma|Urothelial Carcinoma Less << PHASE2 WITHDRAWN 2018-08-01 -
NCT02432690 Cancer|Ovarian Cancer PHASE2 TERMINATED 2017-01-02 Mayo Clinic, Rochester, Minnes... More >>ota, 55905, United States Less <<
NCT01781455 Cancer, Advanced Solid Tumors PHASE1 COMPLETED 2025-06-20 Mayo Clinic Cancer Center, Sco... More >>ttsdale, Scottsdale, Arizona, 85259, United States|Rocky Mountain Cancer Centers, Denver, Colorado, 80218, United States|Indiana University, Indianapolis, Indiana, 46202, United States|Massachusetts General Hospital, Boston, Massachusetts, 02114, United States|Beth Israel Deaconess Medical Center, Boston, Massachusetts, 02215, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02215, United States|University of Michigan Comprehensive Cancer Center, Ann Arbor, Michigan, 48109, United States|Mayo Clinic Cancer Center, Rochester, Rochester, Minnesota, 55905, United States|Comprehensive Cancer Centers of Nevada, Las Vegas, Nevada, 89169, United States|Institute for Translational Oncology Research, Greenville Hospital System, Greenville, South Carolina, 29605, United States|Texas Oncology- Baylor Charles A. Sammons Cancer Center, Dallas, Texas, 75246, United States|Texas Oncology- Fort Worth, Fort Worth, Texas, 76104, United States|Cancer Care Centers of South Texas, San Antonio, Texas, 78217, United States|Cancer Care Centers of South Texas - HOAST, San Antonio, Texas, 78229, United States|Texas Oncology- Tyler, Tyler, Texas, 75702, United States|Virginia Cancer Specialists, P.C., Fairfax, Virginia, 22031, United States|Virginia Oncology Associates, Norfolk, Virginia, 23502, United States|Yakima Memorial Hostpial/North Star Lodge, Yakima, Washington, 98902, United States|Ottawa Hospital Cancer Centre, Ottawa, Ontario, K1H 8L6, Canada Less <<
NCT02232633 Hepatocellular Carcinoma|Chola... More >>ngiocarcinoma Less << PHASE2 COMPLETED 2017-12-14 University of Calgary, Calgary... More >>, Alberta, T2N 4N2, Canada|The Ottawa Hospital Cancer Centre, Ottawa, Ontario, K1H 8L6, Canada|Princess Margaret Hospital, Toronto, Ontario, Canada Less <<
NCT02232620 Gastrointestinal Stromal Tumor... More >>s Less << PHASE2 TERMINATED 2017-07-25 Princess Margaret Cancer Centr... More >>e, Toronto, Ontario, M5G 2M9, Canada 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
 

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