1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. VEGFR
    Autophagy

Brivanib (Synonyms: BMS-540215)

Cat. No.: HY-10337
Handling Instructions

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

For research use only. We do not sell to patients.
Brivanib Chemical Structure

Brivanib Chemical Structure

CAS No. : 649735-46-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $121 In-stock
5 mg $110 In-stock
10 mg $180 In-stock
50 mg $590 In-stock
100 mg $990 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Brivanib:

  • Biological Activity

  • Protocol

  • Technical Information

  • References

Description

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

IC50 & Target

IC50: 25 nM (VEGFR2)

In Vitro

Brivanib inhibits VEGFR1 and FGFR-1 with IC50 of 0.38 μM and 0.148 μM. Brivanib is not sensitive to PDGFRβ, EGFR, LCK, PKCα or JAK-3 with IC50 all above 1900 nM. Brivanib could inhibit the proliferation of VEGF-stimulated HUVECs with IC50 of 40 nM, compared to 276 nM in FGF-stimulated HUVECs. On the other hand, brivanib exhibits low activity to tumor cell lines[1]. Brivanib doses ≤20 µM paradoxically enhances FGF-induced LX-2 cell proliferation, whereas higher brivanib doses (≥30 µM) inhibits LX-2 cell proliferation. The inhibitory effect of brivanib on liver fibrosis is not through inhibition of TGF-β1-induced stellate cell activation, and is possibly through inhibition of PDGF-BB-induced stellate cell activation[3].

In Vivo

Brivanib displays antitumor activities in H3396 xenograft in athymic mice. At a dose of 60 and 90 mg/kg (p.o.), brivanib completely inhibits the tumor growth, with TGI of 85% and 97%, respectively[1]. Moreover, brivanib significantly suppresses tumor growth in Hepatocellular carcinoma (HCC) xenografts, which due to the decrease in phosphorylation of VEGFR2. The results show that the tumor weights in 06-0606 xenograft mice are 55% and 13%, compared with the controls at a dose of 50 mg/kg and 100 mg/kg. Brivanib is suggested to be efficient in treatment of HCC[2]. Brivanib (50 mg/kg, p.o.) attenuates liver fibrosis and stellate cell activation induced by BDL in mice. Brivanib inhibits growth factor and growth factor receptor mRNA expression in sham control animals but shows variable effects in bile duct ligated animals[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00300027 Bristol-Myers Squibb Gastrointestinal Neoplasms April 2006 Phase 1
NCT00437437 Bristol-Myers Squibb Tumors May 2000 Phase 1
NCT01540461 Bristol-Myers Squibb Hepatocellular Carcinoma March 2012 Phase 1
NCT00437424 Bristol-Myers Squibb Carcinoma, Hepatocellular July 2007 Phase 1
NCT00355238 Bristol-Myers Squibb Hepatocellular Carcinoma (HCC) December 2006 Phase 2
NCT01267253 Gynecologic Oncology Group|National Cancer Institute (NCI) Cervical Adenocarcinoma|Cervical Adenosquamous Carcinoma|Cervical Squamous Cell Carcinoma, Not Otherwise Specified|Persistent Disease|Recurrent Cervical Carcinoma April 2011 Phase 2
NCT01108705 Bristol-Myers Squibb Carcinoma, Hepatocellular May 2010 Phase 3
NCT00888173 Gynecologic Oncology Group|National Cancer Institute (NCI) Endometrial Adenocarcinoma|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 July 2009 Phase 2
NCT01367275 M.D. Anderson Cancer Center|Bristol-Myers Squibb Colorectal Cancer|Colorectal Adenocarcinoma August 2011 Phase 2
NCT00825955 Bristol-Myers Squibb Liver Cancer February 2009 Phase 3
NCT00435669 Bristol-Myers Squibb Tumors September 2007 Phase 1
NCT00908752 Bristol-Myers Squibb Hepatocellular Carcinoma July 20, 2009 Phase 3
NCT00390936 Bristol-Myers Squibb Solid Tumors October 2007 Phase 1
NCT00633789 Bristol-Myers Squibb Advanced Non-small Cell Lung Cancer|Transitional Cell Carcinoma|Soft Tissue Sarcoma|Gastric/Esophageal Adenocarcinoma|Pancreatic Cancer Including Ampulla of Vater June 2008 Phase 2
NCT00640471 NCIC Clinical Trials Group|Canadian Cancer Trials Group Colorectal Cancer May 2008 Phase 3
NCT00798252 Bristol-Myers Squibb Advanced Cancer March 2009 Phase 1
NCT00858871 Bristol-Myers Squibb Hepato Cellular Carcinoma (HCC) May 2009 Phase 3
NCT01253668 Abramson Cancer Center of the University of Pennsylvania Male and Female Subjects 18 Years of Age and Older With Metastatic Renal Cell Carcinoma. Eligible Patients Must Have Undergone and Failed Prior Treatment. November 2010 Phase 2
NCT01046864 Bristol-Myers Squibb Gastro-Intestinal Cancer February 2010 Phase 1
NCT00207051 Bristol-Myers Squibb Colorectal Cancer January 2006 Phase 1
NCT00594984 Bristol-Myers Squibb Metastatic Colorectal Cancer (MCRC) May 2008 Phase 1|Phase 2
NCT00207103 Bristol-Myers Squibb Tumors|Neoplasm Metastasis September 2004 Phase 1
NCT00300027 Bristol-Myers Squibb Gastrointestinal Neoplasms April 2006 Phase 1
NCT00437437 Bristol-Myers Squibb Tumors May 2000 Phase 1
NCT01540461 Bristol-Myers Squibb Hepatocellular Carcinoma March 2012 Phase 1
NCT00437424 Bristol-Myers Squibb Carcinoma, Hepatocellular July 2007 Phase 1
NCT00355238 Bristol-Myers Squibb Hepatocellular Carcinoma (HCC) December 2006 Phase 2
NCT01267253 Gynecologic Oncology Group|National Cancer Institute (NCI) Cervical Adenocarcinoma|Cervical Adenosquamous Carcinoma|Cervical Squamous Cell Carcinoma, Not Otherwise Specified|Persistent Disease|Recurrent Cervical Carcinoma April 2011 Phase 2
NCT01108705 Bristol-Myers Squibb Carcinoma, Hepatocellular May 2010 Phase 3
NCT00888173 Gynecologic Oncology Group|National Cancer Institute (NCI) Endometrial Adenocarcinoma|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 July 2009 Phase 2
NCT01367275 M.D. Anderson Cancer Center|Bristol-Myers Squibb Colorectal Cancer|Colorectal Adenocarcinoma August 2011 Phase 2
NCT00825955 Bristol-Myers Squibb Liver Cancer February 2009 Phase 3
NCT00435669 Bristol-Myers Squibb Tumors September 2007 Phase 1
NCT00908752 Bristol-Myers Squibb Hepatocellular Carcinoma July 20, 2009 Phase 3
NCT00390936 Bristol-Myers Squibb Solid Tumors October 2007 Phase 1
NCT00633789 Bristol-Myers Squibb Advanced Non-small Cell Lung Cancer|Transitional Cell Carcinoma|Soft Tissue Sarcoma|Gastric/Esophageal Adenocarcinoma|Pancreatic Cancer Including Ampulla of Vater June 2008 Phase 2
NCT00640471 NCIC Clinical Trials Group|Canadian Cancer Trials Group Colorectal Cancer May 2008 Phase 3
NCT00798252 Bristol-Myers Squibb Advanced Cancer March 2009 Phase 1
NCT00858871 Bristol-Myers Squibb Hepato Cellular Carcinoma (HCC) May 2009 Phase 3
NCT01253668 Abramson Cancer Center of the University of Pennsylvania Male and Female Subjects 18 Years of Age and Older With Metastatic Renal Cell Carcinoma. Eligible Patients Must Have Undergone and Failed Prior Treatment. November 2010 Phase 2
NCT01046864 Bristol-Myers Squibb Gastro-Intestinal Cancer February 2010 Phase 1
NCT00207051 Bristol-Myers Squibb Colorectal Cancer January 2006 Phase 1
NCT00594984 Bristol-Myers Squibb Metastatic Colorectal Cancer (MCRC) May 2008 Phase 1|Phase 2
NCT00207103 Bristol-Myers Squibb Tumors|Neoplasm Metastasis September 2004 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.6999 mL 13.4996 mL 26.9993 mL
5 mM 0.5400 mL 2.6999 mL 5.3999 mL
10 mM 0.2700 mL 1.3500 mL 2.6999 mL
Cell Assay
[3]

Viability is measured in LX-2 cells using the Cell Counting Kit-8 (CCK-8). Using 96-well plates with 2,000 cells per well, HSCs are incubated in 10% FBS-supplemented DMEM for 24 hours, followed by starvation in serum-free media. After 24 hours of starvation, brivanib is added at different doses. Two hours later, 5 ng/mL PDGF-BB is added. The cells are incubated for an additional 72 hours and cell viability is measured. Each experiment is performed in three replicates at least four times. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Male mice 4-6 weeks of age are treated 3 times a week with a total of 12 intraperitoneal (i.p.) injections of 150 mL/kg TAA. At the onset of TAA treatment, placebo or brivanib (25 or 50 mg/kg) is administered orally on 5 consecutive days with weekend breaks. The animals are sacrificed 4 weeks after the start of the injections. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

370.38

Formula

C₁₉H₁₉FN₄O₃

CAS No.

649735-46-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 50 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Brivanib
Cat. No.:
HY-10337
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