Brivanib

• Description:

  Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β[1].

• Product Name Alternative:

  BMS-540215

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  Autophagy; VEGFR

• Type:

  Reference compound

• Related Pathways:

  Autophagy; Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Brivanib.html

• Concentration:

  10mM

• Purity:

  99.92

• Solubility:

  DMSO : ≥ 50 mg/mL

• Smiles:

  FC1=C(OC2=NC=NN3C2=C(C(OC[C@H](O)C)=C3)C)C=CC4=C1C=C(C)N4

• Molecular Formula:

  C19H19FN4O3

• Molecular Weight:

  370.38

• Precautions:

  H302, H315, H319, H335

• References & Citations:

  [1]Bhide RS, et al. 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. J Med Chem, 2006, 49 (7), 2143-2146.|[2]Huynh H, et al. Brivanib alaninate, a dual inhibitor of vascular endothelial growth factor receptor and fibroblast growth factor receptor tyrosine kinases, induces growth inhibition in mouse models of human hepatocellular carcinoma. Clin Cancer Res, 2008, |[3]Nakamura I, et al. Correction: Brivanib Attenuates Hepatic Fibrosis In Vivo and Stellate Cell Activation In Vitro by Inhibition of FGF, VEGF and PDGF Signaling. PLoS One. 2015 Nov 3;10 (11) :e0142355.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 3

• Isoform:

  VEGFR2/KDR/Flk-1

• CAS Number:

  [649735-46-6]