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Chemical Structure| 649735-46-6 Chemical Structure| 649735-46-6

Structure of Brivanib
CAS No.: 649735-46-6

Chemical Structure| 649735-46-6

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Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but > 240-fold against PDGFR-β.

Synonyms: BMS-540215

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Product Details of Brivanib

CAS No. :649735-46-6
Formula : C19H19FN4O3
M.W : 370.38
SMILES Code : C[C@@H](O)COC1=CN2N=CN=C(OC3=C(F)C4=C(NC(C)=C4)C=C3)C2=C1C
Synonyms :
BMS-540215
MDL No. :MFCD13194684
InChI Key :WCWUXEGQKLTGDX-LLVKDONJSA-N
Pubchem ID :11234052

Safety of Brivanib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H317
Precautionary Statements:P280

Related Pathways of Brivanib

RTK

Isoform Comparison

Biological Activity

Target
  • VEGFR1

    VEGFR1, IC50:380 nM

  • VEGFR2

    VEGFR2, IC50:25 nM

    Flk1, IC50:25 nM

  • FGFR1

    FGFR1, IC50:148 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2-SR cells 2.5, 5 μM 48 hrs/72 hrs Brivanib, as a positive control, reduced the viability of HepG2-SR cells and induced apoptosis. PMC9120623
HepG2 60 μM 72 h To evaluate the effect of Notch3 silencing on Brivanib response, results showed that Notch3 silencing enhanced the apoptotic effect of Brivanib on HepG2 cells. PMC6461893
Huh7 60 μM 72 h To evaluate the effect of Notch3 silencing on Brivanib response, results showed that Notch3 silencing enhanced the apoptotic effect of Brivanib on Huh7 cells. PMC6461893
Hep3B 60 μM 72 h To evaluate the effect of Notch3 silencing on Brivanib response, results showed that Notch3 silencing did not significantly enhance the apoptotic effect of Brivanib on Hep3B cells. PMC6461893

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MCF-7 E2 tumor model Oral 0.05 mg/g and 0.1 mg/g Daily for 6 weeks To evaluate the effect of Brivanib Alaninate on the growth of MCF-7 E2 tumors. Results showed that the high dose (0.1 mg/g) significantly inhibited tumor growth, while the low dose (0.05 mg/g) had no significant effect. PMC2927957
mice RIP1-Tag2 transgenic mice oral 75 mg/kg once daily for 5.5 weeks To evaluate the therapeutic efficacy of Brivanib in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors (PNET). Results showed that Brivanib treatment significantly extended the lifespan of the mice and maintained tumor stasis during the 5.5 weeks of therapy. PMC3156934
BALB/c- nu/nu mice HepG2-SR hepatoma model Oral administration 100 mg/kg Once daily for 15 consecutive days Brivanib, as a positive control, significantly inhibited HepG2-SR tumor growth. PMC9120623
Mice Liver fibrosis models induced by bile duct ligation (BDL), chronic carbon tetrachloride (CCl4), and chronic thioacetamide (TAA) Oral 25 mg/kg, 50 mg/kg, 100 mg/kg Administered for 5 consecutive days with 2 days off on weekends, lasting for 4 weeks To evaluate the effect of brivanib on liver fibrosis, results showed that brivanib significantly reduced liver fibrosis and decreased the expression of collagen Iα1 and α-smooth muscle actin in the liver. PMC3977817
Rats DENA-induced HCC model Oral gavage 60 mg/kg Once daily for 15 days To evaluate the effect of Brivanib combined with Notch3 silencing on the HCC model, results showed that Notch3 silencing significantly enhanced the inhibitory effect of Brivanib on tumor growth. PMC6461893

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00594984 Metastatic Colorectal Cancer (... More >>MCRC) Less << Phase 1 Phase 2 Completed - United States, California ... More >> Usc/Norris Comprehensive Cancer Center Hospital Los Angeles, California, United States, 90033 Usc/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, Kentucky James Graham Brown Cancer Center Louisville, Kentucky, United States, 40202 United States, Missouri Washington University Saint Louis, Missouri, United States, 63110 Argentina Local Institution Buenos Aires, Argentina, C1426ANZ Denmark Local Institution Odense C, Denmark, 5000 Italy Local Institution Meldola Fc, Italy, 47014 Local Institution Milano, Italy, 20141 Korea, Republic of Local Institution Seoul, Korea, Republic of, 135-710 Spain Local Institution Madrid, Spain, 28050 Sweden Local Institution Stockholm, Sweden, 17176 Local Institution Uppsala, Sweden, 75185 Less <<
NCT00300027 Gastrointestinal Neoplasms Phase 1 Terminated - United States, Arkansas ... More >> Local Institution Little Rock, Arkansas, United States United States, California Local Institution Los Angeles, California, United States United States, District of Columbia Local Institution Washington, District of Columbia, United States United States, Iowa Local Institution Iowa City, Iowa, United States United States, North Carolina Local Institution Durham, North Carolina, United States United States, Texas Local Institution Temple, Texas, United States Less <<
NCT01046864 Gastro-Intestinal Cancer Phase 1 Completed - United States, California ... More >> Usc/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, Texas Texas Oncology Dallas, Texas, United States, 75246 Scott & White Memorial Hospital And Clinic Temple, Texas, United States, 76508 Canada, Alberta Local Institution Edmonton, Alberta, Canada, T6G 1Z2 Canada, Ontario Local Institution Ottawa, Ontario, Canada, K1H 8L6 France Local Institution Villejuif Cedex, France, 94800 Less <<
NCT00207103 Tumors Neopla... More >>sm Metastasis Less << Phase 1 Completed - United States, California ... More >> Premiere Oncology Santa Monica, California, United States, 90404 United States, Indiana Indiana University Med Center Indianapolis, Indiana, United States, 46202 United States, Wisconsin University Of Wisconsin Comprehensive Center Madison, Wisconsin, United States, 53792 Canada, Alberta Local Institution Edmonton, Alberta, Canada, T6G 1Z2 Canada, Ontario Local Institution Ottawa, Ontario, Canada, K1H 1C4 Italy Local Institution Milano, Italy, 20141 United Kingdom Local Institution Middlesex, Greater London, United Kingdom, HA6 2RN Local Institution Manchester, Greater Manchester, United Kingdom, M20 4BX Less <<
NCT00858871 Hepato Cellular Carcinoma (HCC... More >>) Less << Phase 3 Completed - -
NCT00798252 Advanced Cancer Phase 1 Completed - United States, California ... More >> Usc/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, Massachusetts Dana Farber Cancer Institute Boston, Massachusetts, United States, 02215 United States, Michigan Wayne State University Detroit, Michigan, United States, 48201 Canada, Alberta Local Institution Edmonton, Alberta, Canada, T6G 1Z2 Canada, Ontario Local Institution Toronto, Ontario, Canada, M5G 2M9 Less <<
NCT01253668 Renal Cell Carcinoma Phase 2 Completed - United States, Pennsylvania ... More >> Abramson Cancer Center of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 Less <<
NCT00390936 Solid Tumors PHASE1 COMPLETED 2025-03-10 Local Institution, Sunto-Gun, ... More >>Shizuoka, 411-8777, Japan Less <<
NCT00640471 Colorectal Cancer Phase 3 Completed - -
NCT00908752 Hepatocellular Carcinoma Phase 3 Completed - -
NCT00207051 Colorectal Cancer Phase 1 Completed - United States, California ... More >> Usc/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, District of Columbia Georgetn Univ Lombardi Can Ctr Washington, District of Columbia, United States, 20007 United States, Florida University Of Miami Miller School Of Medicine Miami, Florida, United States, 33010 H. Lee Moffitt Cancer Center Tampa, Florida, United States, 33612 United States, Michigan Karmanos Cancer Institute Detroit, Michigan, United States, 48201 Canada, Ontario Local Institution Hamilton, Ontario, Canada, L8V 2C5 Local Institution Toronto, Ontario, Canada, M5G 2M9 Netherlands Local Institution Amsterdam, Netherlands, 1081 HV Less <<
NCT00435669 Tumors Phase 1 Completed - United States, Ohio ... More >> Cleveland Clinic Foundation Cleveland, Ohio, United States, 44195 Less <<
NCT00888173 - Completed - -
NCT01267253 Cervical Adenocarcinoma ... More >> Cervical Adenosquamous Carcinoma Cervical Squamous Cell Carcinoma, Not Otherwise Specified Persistent Disease Recurrent Cervical Carcinoma Less << Phase 2 Active, not recruiting - -
NCT01267253 - Active, not recruiting - -
NCT00355238 Hepatocellular Carcinoma (HCC) Phase 2 Completed - -
NCT00437424 Carcinoma, Hepatocellular PHASE1 COMPLETED 2025-06-10 University Of Alabama At Birmi... More >>ngham, Birmingham, Alabama, 35294, United States|Usc/Norris Comprehensive Cancer Center, Los Angeles, California, 90033, United States|Case Western Reserve University, Clleveland, Ohio, 44106, United States|South Texas Accelerated Research Therapeutics, Llc, San Antonio, Texas, 78229, United States|Local Institution, Sevilla, 41013, Spain Less <<
NCT00633789 Advanced Non-small Cell Lung C... More >>ancer Transitional Cell Carcinoma Soft Tissue Sarcoma Gastric/Esophageal Adenocarcinoma Pancreatic Cancer Including Ampulla of Vater Less << Phase 2 Completed - -
NCT01367275 Colorectal Cancer ... More >> Colorectal Adenocarcinoma Less << Phase 2 Terminated(Sponsor closed stud... More >>y) Less << - United States, Texas ... More >> UT MD Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT01108705 Carcinoma, Hepatocellular Phase 3 Terminated - -
NCT00888173 Endometrial Adenocarcinoma ... More >> Endometrial Clear Cell Adenocarcinoma Endometrial Mixed Adenocarcinoma Endometrial Mucinous Adenocarcinoma Endometrial Serous Adenocarcinoma Endometrial Squamous Cell Carcinoma Endometrial Transitional Cell Carcinoma Endometrial Undifferentiated Carcinoma Recurrent Uterine Corpus Carcinoma Less << Phase 2 Completed - -
NCT03516071 Hepatocellular Carcinoma (HCC) Phase 2 Recruiting May 10, 2019 China, Anhui ... More >> Anhui Provincial Hospital Recruiting Hefei, Anhui, China Contact: Yueyin Pan          China, Guangdong Nanfang Hospital Recruiting Guangzhou, Guangdong, China Contact: Jinlin Hou          Sun Yat-sen University Cancer Center Recruiting Guangzhou, Guangdong, China Contact: Li Xu          China, Heilongjiang Harbin Medical University Cancer Hospital Recruiting Harbin, Heilongjiang, China Contact: Yuxian Bai          China, Henan Henan Cancer Hospital Recruiting Zhengzhou, Henan, China Contact: Xinfang Hou          China, Hunan Hunan Cancer Hospital Recruiting Changsha, Hunan, China Contact: Shanzhi Gu          China, Jiangsu China PLA 81st hospital Recruiting Nanjing, Jiangsu, China Contact: Shukui Qin          China, Jilin The first Hospital of Jilin University Recruiting Changchun, Jilin, China Contact: Wei Li          China, Liaoning Army General Hospital of Shenyang military region Recruiting Shenyang, Liaoning, China Contact: Zhendong Zheng          China, Shanghai Fudan University Shanghai Cancer Center Recruiting Shanghai, Shanghai, China Contact: Zhiqiang Meng          Zhongshan Hospital Recruiting Shanghai, Shanghai, China Contact: Zhenggang Ren          China, Shanxi Tangdu Hospital Recruiting Xi'an, Shanxi, China Contact: Helong Zhang          China, Sichuan West China Hospital West China School of Medicine Sichuan University Recruiting Chengdu, Sichuan, China Contact: Hong Zhu          China, Tianjin Tianjin Medical University Cancer Institute & Hospital Recruiting Tianjin, Tianjin, China Contact: Tianqiang Song          China, Zhejiang Zhejiang Cancer Hospital Recruiting Hangzhou, Zhejiang, China Contact: Jieer Ying Less <<
NCT00825955 Liver Cancer Phase 3 Terminated(Efficacy endpoint m... More >>et, however, overall experimental dosing regimen is not considered optimal to support further clinical development in this patient population) Less << - -
NCT01540461 Hepatocellular Carcinoma PHASE1 COMPLETED 2025-11-13 Local Institution, Beijing, Be... More >>ijing, 100071, China|Local Institution, Ha Erbin, Heilongjiang, 150040, China|Local Institution, Nanjing, Jiangsu, 210002, China Less <<
NCT00437437 Tumors PHASE1 COMPLETED 2025-02-13 Dana-Farber Harvard Cancer Car... More >>e, Boston, Massachusetts, 02115, United States|Wayne State University, Detroit, Michigan, 48201-2194, United States|Duke University Medical Center-Dept Of Medicine, Durham, North Carolina, 27710, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.50mL

2.70mL

1.35mL

27.00mL

5.40mL

2.70mL

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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