Structure of Brivanib
CAS No.: 649735-46-6
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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
4.5
*For Research Use Only !
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| 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 |
| GHS Pictogram: |
|
| Signal Word: | Warning |
| Hazard Statements: | H302-H317 |
| Precautionary Statements: | P280 |
| Target |
|
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. | J Ginseng Res. 2022 May;46(3):418-425. |
| 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. | Br J Cancer. 2019 Mar;120(6):601-611. |
| 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. | Br J Cancer. 2019 Mar;120(6):601-611. |
| 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. | Br J Cancer. 2019 Mar;120(6):601-611. |
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. | Eur J Cancer. 2010 Jun;46(9):1537-53 |
| 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. | Clin Cancer Res. 2011 Aug 15;17(16):5299-310 |
| 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. | J Ginseng Res. 2022 May;46(3):418-425. |
| 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. | PLoS One. 2014 Apr 7;9(4):e92273 |
| 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. | Br J Cancer. 2019 Mar;120(6):601-611. |
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 << |
Tags: Brivanib | BMS-540215 | BMS540215 | BMS 540215 | VEGFR Inhibitor | VEGFR | VEGFR2 Inhibitor | VEGFR1 Inhibitor | FGFR1 Inhibitor | PDGFR-β Inhibitor | Autophagy | Vascular endothelial growth factor receptor | angiogenesis | VEGF receptor | endothelial cell proliferation | anti-angiogenic | 649735-46-6
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Response | |
| Code | Phrase |
| P301 | IF SWALLOWED: |
| P304 | IF INHALED: |
| P305 | IF IN EYES: |
| P306 | IF ON CLOTHING: |
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| H242 | Heating may cause a fire |
| H250 | Catches fire spontaneously if exposed to air |
| H251 | Self-heating; may catch fire |
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| H260 | In contact with water releases flammable gases which may ignite spontaneously |
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| H290 | May be corrosive to metals |
Health hazards | |
| Code | Phrase |
| H300 | Fatal if swallowed |
| H301 | Toxic if swallowed |
| H302 | Harmful if swallowed |
| H303 | May be harmful if swallowed |
| H304 | May be fatal if swallowed and enters airways |
| H305 | May be harmful if swallowed and enters airways |
| H310 | Fatal in contact with skin |
| H311 | Toxic in contact with skin |
| H312 | Harmful in contact with skin |
| H313 | May be harmful in contact with skin |
| H314 | Causes severe skin burns and eye damage |
| H315 | Causes skin irritation |
| H316 | Causes mild skin irritation |
| H317 | May cause an allergic skin reaction |
| H318 | Causes serious eye damage |
| H319 | Causes serious eye irritation |
| H320 | Causes eye irritation |
| H330 | Fatal if inhaled |
| H331 | Toxic if inhaled |
| H332 | Harmful if inhaled |
| H333 | May be harmful if inhaled |
| H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
| H335 | May cause respiratory irritation |
| H336 | May cause drowsiness or dizziness |
| H340 | May cause genetic defects |
| H341 | Suspected of causing genetic defects |
| H350 | May cause cancer |
| H351 | Suspected of causing cancer |
| H360 | May damage fertility or the unborn child |
| H361 | Suspected of damaging fertility or the unborn child |
| H361d | Suspected of damaging the unborn child |
| H362 | May cause harm to breast-fed children |
| H370 | Causes damage to organs |
| H371 | May cause damage to organs |
| H372 | Causes damage to organs through prolonged or repeated exposure |
| H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
| Code | Phrase |
| H400 | Very toxic to aquatic life |
| H401 | Toxic to aquatic life |
| H402 | Harmful to aquatic life |
| H410 | Very toxic to aquatic life with long-lasting effects |
| H411 | Toxic to aquatic life with long-lasting effects |
| H412 | Harmful to aquatic life with long-lasting effects |
| H413 | May cause long-lasting harmful effects to aquatic life |
| H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
Sorry,this product has been discontinued.
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