Brivanib (alaninate)

• Description:

  Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ[1].

• Product Name Alternative:

  BMS-582664

• UNSPSC:

  12352005

• Hazard Statement:

  H302-H360

• 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-alaninate.html

• Purity:

  99.45

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  O=C(O[C@@H](COC1=CN2C(C(OC3=C(C4=C(NC(C)=C4)C=C3)F)=NC=N2)=C1C)C)[C@@H](N)C

• Molecular Formula:

  C22H24FN5O4

• Molecular Weight:

  441.46

• Precautions:

  P264-P270-P280-P330-P405-P501

• 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, 14 (19), 6146-6153.|[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:

  [649735-63-7]