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Chemical Structure| 475108-18-0 Chemical Structure| 475108-18-0

Structure of Tivozanib
CAS No.: 475108-18-0

Chemical Structure| 475108-18-0

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Tivozanib is an inhibitor of VEGFR1, VEGFR2 and VEGFR3 with IC50s of 30 nM, 6.5 nM, 15 nM, respectively. It can also inhibit PDGFR and c-Kit.

Synonyms: KRN951; AV-951; KRN-951, Tivozanib

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Product Details of Tivozanib

CAS No. :475108-18-0
Formula : C22H19ClN4O5
M.W : 454.86
SMILES Code : O=C(NC1=NOC(C)=C1)NC2=CC=C(OC3=CC=NC4=CC(OC)=C(OC)C=C34)C=C2Cl
Synonyms :
KRN951; AV-951; KRN-951, Tivozanib
MDL No. :MFCD15146788
InChI Key :SPMVMDHWKHCIDT-UHFFFAOYSA-N
Pubchem ID :9911830

Safety of Tivozanib

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

Related Pathways of Tivozanib

RTK

Isoform Comparison

Biological Activity

Target
  • VEGFR1

    VEGFR1, IC50:30 nM

  • VEGFR3

    VEGFR3, IC50:15 nM

  • VEGFR2

    VEGFR2, IC50:6.5 nM

  • PDGFRβ

    PDGFRβ, IC50:49 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Zebrafish embryo 1 μM and 0.5 μM 96 h Evaluate the effect of Tivozanib on angiogenesis in zebrafish embryos, results showed that Tivozanib significantly inhibited angiogenesis PMC11826465

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Zebrafish Brain injury model Intralesional injection 2 μM Single injection, lasting 3 days Evaluate the effect of Tivozanib on angiogenesis and neurogenesis after brain injury, results showed that Tivozanib significantly inhibited angiogenesis and neurogenesis PMC11826465

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03419572 - Recruiting January 5, 2021 -
NCT00970411 Solid Tumors PHASE1 COMPLETED 2025-04-16 Shizuoka, Japan
NCT01058655 Gastrointestinal Cancer Phase 1 Phase 2 Completed - United States, Massachusetts ... More >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02115 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 Less <<
NCT01631097 Hepatic Impairment Phase 1 Completed - United States, Florida ... More >> Miami, Florida, United States Orlando, Florida, United States Less <<
NCT01058655 - Completed - -
NCT01478594 Colorectal Cancer Phase 2 Completed - -
NCT01030783 Advanced Renal Cell Carcinoma Phase 3 Completed - -
NCT01076010 Advanced Renal Cell Carcinoma Phase 3 Completed - -
NCT01835223 Advanced Adult Hepatocellular ... More >>Carcinoma Non-Resectable Hepatocellular Carcinoma Less << Phase 1 Phase 2 Active, not recruiting December 1, 2019 United States, New York ... More >> Roswell Park Cancer Institute Buffalo, New York, United States, 14263 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 Less <<
NCT01478594 - Completed - -
NCT01745367 Triple Negative Breast Cancer Phase 2 Terminated(low enrollment) - -
NCT00502307 Carcinoma, Renal Cell Phase 2 Completed - India ... More >> Vellore, Tamil Nadu, India, 632004 Kolkata, India Mumbai, India New Delhi, India Pune, India Russian Federation Astrakhan, Russian Federation Ioshkar-Ola, Russian Federation Kazan, Russian Federation Moscow, Russian Federation, 125284 Moscow, Russian Federation, 129128 Moscow, Russian Federation Novgorod, Russian Federation Obninsk, Russian Federation Pyatigorsk, Russian Federation Rostove-on-Don, Russian Federation Sochi, Russian Federation St. Petersburg, Russian Federation Tomsk, Russian Federation Ufa, Russian Federation Ukraine Cherkassy, Ukraine Dnepropetrovsk, Ukraine Donetsk, Ukraine Kharkov, Ukraine Lviv, Ukraine Uzhgorod, Ukraine Zaporizzhya, Ukraine Less <<
NCT01885949 Prostate Cancer Phase 2 Active, not recruiting June 2019 United States, Massachusetts ... More >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Less <<
NCT01782313 Recurrent Adult Soft Tissue Sa... More >>rcoma Stage III Adult Soft Tissue Sarcoma Stage IV Adult Soft Tissue Sarcoma Less << Phase 2 Completed - United States, Illinois ... More >> Northwestern University Chicago, Illinois, United States, 60611 United States, Iowa University of Iowa Iowa City, Iowa, United States, 52246 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Missouri Washington University Saint Louis, Missouri, United States, 63110 United States, Wisconsin University of Wisconsin Madison, Wisconsin, United States, 53792 Less <<
NCT01210846 Advanced Solid Tumors Phase 1 Completed - United States, Arizona ... More >> TGEN Clinical Research Service at Scottsdale Healthcare Scottsdale, Arizona, United States United States, Florida Florida Cancer Specialists Ft. Myers, Florida, United States United States, Indiana Horizon Oncology Research, Inc. Lafayette, Indiana, United States United States, Louisiana Jayne Gurtler MD, Laura Brinz MD, Angelo Russo MD and Janet Burroff MD APMC Metairie, Louisiana, United States United States, Maryland Associates in Oncology/Hematology Rockville, Maryland, United States United States, Oklahoma Oklahoma University Cancer Institute (OUCI) Oklahoma City, Oklahoma, United States United States, Tennessee Tennessee Onocology Nashville, Tennessee, United States United States, Washington Multicare Research Institute/Tacoma General Hospital Tacoma, Washington, United States Less <<
NCT01782313 - Completed - -
NCT00660153 Colorectal Cancer ... More >> Gastrointestinal Cancer Less << Phase 1 Completed - Netherlands ... More >> University Medical Center Groningen; Internal Medicine, Department of Medical Oncology Groningen, Netherlands Erasmus Medical Center; Department of Medical Oncology Rotterdam, Netherlands Less <<
NCT01673386 Metastatic Renal Cell Carcinom... More >>a Less << Phase 2 Completed - -
NCT02627963 Carcinoma, Renal Cell Phase 3 Active, not recruiting December 2019 -
NCT01728181 Non-small Cell Lung Cancer ... More >> Stage IV Disease EGFR Unknown or Wild-type Less << Phase 1 Phase 2 Withdrawn(Stopped before appro... More >>val due to ineffective drug) Less << March 2016 -
NCT01369433 Solid Tumors Not Applicable Completed - -
NCT00563147 Renal Cell Carcinoma Phase 1 Completed - United States, California ... More >> UCLA Jonsson Comprehensive Cancer Center Los Angeles, California, United States, 90095 Stanford University Stanford, California, United States, 94305 United States, Florida H. Lee Moffitt Cancer Center Tampa, Florida, United States, 33612 United States, Nebraska Nebraska Methodist Hospital Omaha, Nebraska, United States, 68114 United States, Texas The Methodist Hospital Research Institute Houston, Texas, United States, 77030 Less <<
NCT01297244 Renal Cell Carcinoma PHASE2 COMPLETED 2025-10-12 Southern Cancer Center, Mobile... More >>, Alabama, United States|Providence Health and Services, Burbank, California, United States|David Geffen School of Medicine at UCLA, Los Angeles, California, United States|Rocky Mountain Cancer Center, Denver, Colorado, United States|St. Francis Cancer Research Foundation, Beech Grove, Indiana, United States|Cancer Center of Kansas, Wichita, Kansas, United States|Medical Oncology, LLC, Baton Rouge, Louisiana, United States|Dana Farber Cancer Institute, Boston, Massachusetts, United States|Cancer & Hematology Centers of Western Michigan, Grand Rapids, Michigan, United States|North Mississippi Hematology & Oncology Associates, Ltd., Tupelo, Mississippi, United States|Comprehensive Cancer Centers of Nevada & US Oncology Research, Las Vegas, Nevada, United States|Mary Hitchcock Memorial Hospital, NH, Lebanon, New Hampshire, United States|University of North Carolina, Lineberger Comprehensive Cancer Center, Chapel Hill, North Carolina, United States|Ohio State University, Columbus, Ohio, United States|Fox Chase Cancer Center, Philadelphia, Pennsylvania, United States|The Jones Clinic, Germantown, Tennessee, United States|The West Clinic, Memphis, Tennessee, United States|Texas Oncology-Austin North, Austin, Texas, United States|Coastal Bend Cancer Center, Corpus Christi, Texas, 78404, United States|Texas Oncology-Baylor, Charles A. Sammons Cancer Center, Dallas, Texas, United States|BC Cancer Agency Vancouver Centre, Vancouver, British Columbia, Canada|Juravinski Cancer Center, Hamilton, Ontario, Canada|Princess Margaret Hospital, Toronto, Ontario, Canada|Sunnybrook Odette Cancer Center, Toronto, Toronto, Ontario, Canada|Montreal General Hospital, Montreal, Quebec, Canada Less <<
NCT00717340 Metastatic Breast Cancer Phase 1 Completed - United States, Massachusetts ... More >> Dana Farber Cancer Institute, Inc. Boston, Massachusetts, United States, 02115 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 Germany Universitaetsklinikum Essen Essen, Germany, D-45147 Less <<
NCT00826878 Carcinoma, Non-Small-Cell Lung Phase 1 Completed - United States, District of Col... More >>umbia Georgetown University Washington, District of Columbia, United States, 20007 United States, Kansas Kansas University Medical Center Kansas City, Kansas, United States, 66160 United States, New York Memorial Sloan-Kettering New York, New York, United States, 10021 Less <<
NCT01846871 Glioblastoma PHASE2 COMPLETED 2025-05-16 Massachusetts General Hospital... More >>, Boston, Massachusetts, 02114, United States Less <<
NCT01306630 Advanced Solid Tumors ... More >> Locally Advanced or Metastatic Breast or Colorectal Cancer Less << Phase 1 Completed - United States, Arizona ... More >> Scottsdale, Arizona, United States, 85258 United States, Florida Fort Myers, Florida, United States, 33908 United States, Tennessee Nashville, Tennessee, United States, 37203 Less <<
NCT01769885 Stage II Renal Cell Cancer ... More >> Stage III Renal Cell Cancer Less << Not Applicable Withdrawn - -
NCT01363778 Healthy Phase 1 Completed - United States, Wisconsin ... More >> Covance Clinical Research Unit, Inc. Madison, Wisconsin, United States, 53704 Less <<
NCT01972516 Ovarian Cancer|Fallopian Tube ... More >>Cancer|Primary Peritoneal Carcinoma Less << PHASE2 TERMINATED 2025-01-16 Dana-Farber Cancer Institute, ... More >>Boston, Massachusetts, 02215, United States Less <<
NCT01972516 Ovarian Cancer|Fallopian Tube ... More >>Cancer|Primary Peritoneal Carcinoma Less << PHASE2 TERMINATED 2025-01-16 Dana-Farber Cancer Institute, ... More >>Boston, Massachusetts, 02215, United States Less <<
NCT01853644 Recurrent Epithelial Ovarian C... More >>ancer|Recurrent Fallopian Tube Cancer|Recurrent Primary Peritoneal Cancer Less << PHASE2 COMPLETED 2021-05-11 Northwestern University, Chica... More >>go, Illinois, 60611, United States|CDH-Delnor Health System - Northwestern Medicine Cancer Center, Warrenville, Illinois, 60555, United States Less <<
NCT01363804 Healthy PHASE1 COMPLETED 2025-07-11 Covance Clinical Research Unit... More >>, Inc., Daytona Beach, Florida, 32117, United States Less <<
NCT01834183 Renal Cell Carcinoma Phase 2 Withdrawn(Sponsor Aveo has wit... More >>hdrawn support for this trial.) Less << - United States, Massachusetts ... More >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 Brigham and Women's Hospital Boston, Massachusetts, United States, 02215 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02215 Less <<
NCT01807156 Hepatocellular Cancer PHASE2 TERMINATED 2025-02-15 Emory University, Winship Canc... More >>er Institute, Atlanta, Georgia, 30322, United States Less <<
NCT01316848 Food Effect of Tivozanib in He... More >>alth Subjects Less << Phase 1 Completed - United States, Texas ... More >> Covance Clinical Research Unit, Inc. Dallas, Texas, United States Less <<
NCT01807156 Hepatocellular Cancer PHASE2 TERMINATED 2025-02-15 Emory University, Winship Canc... More >>er Institute, Atlanta, Georgia, 30322, United States Less <<
NCT03136627 Carcinoma, Renal Cell Phase 1 Phase 2 Active, not recruiting December 2018 France ... More >> Bordeaux Hospital University Center (CHU) Bordeaux, France Center Léon Bérard Lyon, France Institut Paoli-Calmettes Marseille, France Centre Paul Strauss Strasbourg, France, 67065 Institut Gustave Roussy Villejuif, France, 94805 Less <<
NCT04645160 Cholangiocarcinoma|Bile Duct N... More >>eoplasm|Biliary Tract Malignancy Less << PHASE1|PHASE2 RECRUITING 2027-12-31 National Institutes of Health ... More >>Clinical Center, Bethesda, Maryland, 20892, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

10.99mL

2.20mL

1.10mL

21.98mL

4.40mL

2.20mL

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

References

 

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