In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Brivanib is an ATP competitive inhibitor of human VEGFR-2 with IC50 value of 25nM .
Brivanib is a selective RTK inhibitor that targets signaling via VEGFR2 and 3, and FGFR1, 2 and 3. Targeting both VEGF and FGF signaling pathways inhibits tumor growth in RT2 mice, with VEGF signaling predominating in initiation of tumor angiogenesis, Currently, brivanib therapy is being evaluated in phase III clinical trials in colorectal carcinoma and hepatocellular carcinoma (HCC) and in phase II trials for numerous indications including brivanib second-line therapy following sorafenib failure .
Brivanib has moderate potency against VEGFR-1 and FGFR-1 and good selectivity against PDGFR-β. In the preclinical in vivo mouse models, it is also found to be a good inhibitor of Flk-1, the mouse homologue of VEGFR-2 with IC50 value of 89 nM. Brivanib is reported to inhibit the proliferation of human umbilical vein endothelial cells (HUVEC) with potency against VEGF-stimulated HUVECs and FGF-stimulated HUVECs. The IC50 values are 40 nM and 276nM respectively. When tested against human tumor cell lines, Brivanib shows lower antiproliferative potency. In particular, activity was low against the cell line used in the in vivo tumor xenograft mouse efficacy model (H3396) .
 Rajeev S. Bhide, Zhen-Wei Cai, Yong-Zheng Zhang, Ligang Qian, Donna Wei, Stephanie Barbosa, Louis J. Lombardo, Robert M. Borzilleri, Xiaoping Zheng, Laurence I. Wu, Joel C. Barrish, Soong-Hoon Kim, Kenneth Leavitt, Arvind Mathur, Leslie Leith, Sam Chao, Barri Wautlet, Steven Mortillo, Robert Jeyaseelan Sr., Daniel Kukral, John T. Hunt, Amrita Kamath, Aberra Fura, Viral Vyas, Punit Marathe, Celia D’Arienzo, George Derbin, and Joseph Fargnoli. Discovery and Preclinical Studies of (R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol (BMS-540215), an In Vivo Active Potent VEGFR-2 Inhibitor. Journal of Medicinal Chemistry. 2006, 49 (7): 2143-2146.
 Elizabeth Allen, Ian B. Walters, and Douglas Hanahan. Brivanib, a Dual FGF/VEGF Inhibitor, Is Active Both First and Second Line against Mouse Pancreatic Neuroendocrine Tumors Developing Adaptive/Evasive Resistance to VEGF Inhibition. Clinical Cancer Research. 2011 (17): 5299-5310.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥18.5mg/mL in DMSO|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|
|Description||Brivanib is an ATP-competitive inhibitor of human VEGFR-2 with IC50 value of 25 nM .|